Journal articles: 'Derivatives of 5'

1

Drašar, Pavel, and Jiří Beránek. "2',3'-O-Carbonyl derivatives of 6-azauridine in the synthesis of its 5-substituted and 5'-deoxy derivatives." Collection of Czechoslovak Chemical Communications 52, no. 8 (1987): 2070–82. http://dx.doi.org/10.1135/cccc19872070.

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Preparation of 2',3'-O-carbonyl derivatives of 5'-deoxy-6-azauridine and 6-azauridine using 1,1'-carbonyldiimidazole has been elaborated. 5'-Chloro and 5'-bromo derivatives were prepared by treatment of the 5'-O-mesyl derivative with quaternary ammonium halides, 5'-chloro derivatives also by direct halogenation with thionyl chloride in hexamethylphosphortriamide or with tetrachloromethane, triphenyl phosphine, and dimethylformamide. Derivatives of 5'-bromo-6-azauridine were reduced with tributyltin hydride to 5'-deoxy-6-azauridine compounds. 6-Azauridine 2',3'-carbonate (IVa) and its 5'-derivatives IVc and IVe on treatment with imidazole in dimethylformamide afforded 2,2'-anhydronucleosides IIIa-IIIc. The 2,2'-anhydro-5'-deoxy compound IIIc underwent alkaline hydrolysis to 5'-deoxy-1-β-D-arabino-pentofuranosyl-6-azauracil (VIa). Treatment of 2,2'-anhydro-5'-deoxy-5'-chloro derivative IIIb with hydrogen chloride led to 2',5'-dichloro derivative If.

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Liu, Xin-Hua, Bao-An Song, Pinaki S. Bhadury, et al. "Novel 5-(3-(Substituted)-4,5-dihydroisoxazol-5-yl)-2-methoxyphenyl Derivatives: Synthesis and Anticancer Activity." Australian Journal of Chemistry 61, no. 11 (2008): 864. http://dx.doi.org/10.1071/ch07395.

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Thirty novel 5-(3-(substituted phenyl)-4,5-dihydroisoxazol-5-yl)-2-methoxyphenyl derivatives were synthesized and evaluated for their antitumour activity. The bioassays showed that the 2-fluorobenzoyl derivative 6ai, the 4-trifluoromethylbenzoyl derivative 6ah, and the 3-trifluoromethyl isoxazole derivatives (6ch and 6ci) were highly effective against PC-3 cells. The IC50 values of 6ah and 6ai against PC-3 cells were 1.5 and 1.8 μg mL–1, respectively.

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3

Krečmerová, Marcela, Hubert Hřebabecký, and Antonín Holý. "Synthesis of 5-Phenylcytosine Nucleoside Derivatives." Collection of Czechoslovak Chemical Communications 61, no. 4 (1996): 645–55. http://dx.doi.org/10.1135/cccc19960645.

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Reaction of silylated 5-phenylcytosine with 1-O-acetyl-2,3,5-tri-O-benzoyl-D-ribose, catalyzed with tin tetrachloride, and subsequent methanolysis afforded 5-phenylcytidine (2). This compound reacted with thionyl chloride in acetonitrile to give cyclic sulfite 3 which on heating in dimethylformamide was converted into 2,2'-anhydro-1-(β-D-arabinofuranosyl)-5-phenylcytosine (4). Analogous reaction of compound 2 with thionyl chloride at reflux gave 5'-chloro-5'-deoxy-2',3'-cyclic sulfite 5. Its heating in dimethylformamide afforded 5'-chloro-2,2'-anhydro derivative 6, mild alkaline hydrolysis led to 5'-chloro-5'-deoxy-5-phenylcytidine (7). Alkaline hydrolysis of 5-phenyl-2,2'-anhydrocytidine (4) gave 5-phenylcytosine arabinoside 8, whereas the 2,2'-anhydro derivative 6 afforded 1-(5-chloro-5-deoxy-β-D-arabinofuranosyl)-5-phenylcytosine (11). At higher temperature, the final reaction product was 2,5'-anhydro-5-phenylcytidine (12). 5'-Chloro-5'-deoxynucleosides 7 and 11 reacted with tri-n-butyl- stannane to give 5'-deoxyribofuranosyl and 5'-deoxyarabinofuranosyl derivatives 15 and 16. 5-Phenylcytidine (2) was converted into the N4-acetate 17 with acetic anhydride. Further reaction with acetic anhydride and hydrogen bromide in acetic acid afforded a mixture of peracetylated 2'-bromo and 3'-bromo derivatives 18 and 19. Reaction with Zn/Cu couple gave 5'-O-acetyl-5-phenyl-2',3'-didehydro derivative 20 and 2',3',5'-tri-O-acetyl-5-phenylcytidine (21). Compound 20 was deblocked to 1-(2,3-dideoxy-β-D-glycero-pent-2-enofuranosyl)-5-phenylcytosine (22). Catalytic hydrogenation of compound 20 over palladium and subsequent deblocking of the protected 2',3'-dideoxy derivative 23 gave 1-(2,3-dideoxy-β-D-glycero-pentofuranosyl)-5-phenylcytosine (24).

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4

Persson, T., A. B. Hörnfeldt, S. Gronowitz та N. G. Johansson. "Synthesis of Mimics to 5-(2″-thienyl)-2′,3′-β-Dideoxyuridine Triphosphate". Antiviral Chemistry and Chemotherapy 7, № 2 (1996): 101–7. http://dx.doi.org/10.1177/095632029600700207.

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A series of 5′-amido derivatives of 5-(2″-thienyl)-2′,3′,5′-β-trideoxyuridine were prepared. The compounds were tested for their inhibition of cellular DNA polymerase α and α HIV-RT. The succinic fumaric and maleic acid derivatives of 5-(2″-thienyl)-2′,3′,5′-β-trideoxyuridine were investigated. None of the compounds inhibited HIV-RT. The fumaric acid derivative inhibited DNA pol α with IC50 33 μg ml−1. The succinic acid derivative was about half as active with IC50 76 μg ml−1. The 5′-N-acyl derivatives also were structurally compared to the monomethyl ester of the triphosphate using the Sybyl program.

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Mistry, Rakesh N., and K. R. Desai. "Studies on Synthesis of Some Novel Heterocyclic Chalcone, Pyrazoline, Pyrimidine - 2 - One, Pyrimidine - 2 - Thione,para-Acetanilide Sulphonyl and Benzoyl Derivatives and their Antimicrobial Activity." E-Journal of Chemistry 2, no. 1 (2005): 30–41. http://dx.doi.org/10.1155/2005/953107.

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1, 2 - Dichloro benzene on chlorosulphonation by chlorosulphonic acid gives 1, 2 - [dichloro] - benzene sulphonyl chloride which on condensation withp–amino acetophenone gives 1-[acetyl] - 1’ , 2’ - [dichloro] - dibenz sulphonamide derivative. This derivative undergo condensation with 2,4- dichloro benzaldehyde gives 1- [3” - (sub. phenyl) - 2” - propene - 1” - one] - 1’ , 2’ - [dichloro] - dibenz sulphonamide derivative which on reaction with 99% hydrazine hydrate and glacial acetic acid gives 1-[acetyl]-3- [1’ , 2’ - (dichloro) - dibenz sulphonamide] -5 - [2” , 4” - dichloro phenyl] - 2 - pyrazoline derivative. This derivative reacts with various substituted aldehydes to give corresponding substituted chalcone derivatives [1(a-j)]. Now, these chalcone derivatives [1(a-j)] on condensation with urea gives corresponding substituted pyrimidine - 2 - one derivatives [2(a-j)] and on condensation with thio-urea gives corresponding substituted pyrimidine- 2 -thione derivatives [3(a-j)]. Further, these chalcone derivatives [1(a-j)] on reaction with 99% hydrazine hydrate gives 1 - [1’ - (H) - 5’ - (sub. phenyl) - 2’ - pyrazoline]- 3 - [1” , 2” - (dichloro) - dibenz sulphonamide] - 5 - [2’’’ , 4’’’ - dichloro phenyl]-2- pyrazoline derivatives [4(a-j)] as an intermediate compounds, which on condensation with p-acetanilide sulphonyl chloride gives corresponding substituted p - acetanilide sulphonyl derivatives [5(a-j)] and on condensation with benzoyl chloride gives corresponding substituted benzoyl derivatives [6(a-j)]. Structure elucidation of synthesised compounds has been made on the basis of elemental analysis, I.R. spectral studies and 1H N.M.R. spectral studies. The antimicrobial activity of the synthesised compounds has been studied against the cultures “Staphylococcus aureus”, “Escherichia coli” and “Candela albicans”.

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Journal, Baghdad Science. "Synthesis and Characterization of New Heterocyclic Compounds from 2, 5- dimercapto -1, 3, 4-Thiadiazole and Their Resins." Baghdad Science Journal 13, no. 2 (2016): 275–88. http://dx.doi.org/10.21123/bsj.13.2.275-288.

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In this research, a new 1, 3, 4-Thiadiazole derivatives have been synthesized by many heterocyclic reactions. Starting from (2, 5 – dimercapto -1, 3, 4-Thiadiazole) a variety of derivatives have been synthesis. Compound (1) was synthesized by the reaction of hydrazine hydrate with carbon disulphide in absolute ethanol. The compound (1) was reacted with 1, 2-dibromoethane in presence of alkali ethanol to give the compound (2). The compound (3) was formed from the reaction of compound (2) with hydrazine hydrate. Schiff base (4) was obtained by reacting of compound (3) with the compound (p-hydroxybenzaldehyde) in absolute ethanol. A variety of phenolic Schiff base (Methylolic, Etheric, and Epoxy) derivatives have been synthesized. Methylolic derivative was synthesized by the reaction of Schiff base (4) with formaldehyde in tetrahydrofuran (THF). Etheric derivative was formed from the reaction of a methylolic Schiff base (5) with saturated alcohol (Methanol).Epoxy derivative was synthesized by the reaction of epichlorohydrine with etheric derivative (6) .The last step of this research was the preparation of a composite material from mixing the Epoxy resin derivative(7), TiO2and morpholine via ring opening. All these derivatives were verified by using (FT-IR, UV) spectra photometer and 1H-NMR spectra. Also, these derivatives were characterized using elemental analysis (C.H.N.S) .

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Engesser, Tobias, and Reinhard Brückner. "Stereoselective Aldol Additions of Glycolic Acid and Its Derivatives." Synthesis 51, no. 08 (2019): 1715–45. http://dx.doi.org/10.1055/s-0037-1611721.

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This review gives a comprehensive overview of aldol additions of glycolic acid derivatives to achiral aldehydes and acetals affording α,β-dihydroxycarboxylic acids or derivatives thereof. The focus is on simple diastereoselectivity. A selection of related aldol additions is also presented: aldol additions of glycolic acid derivatives to ketones with two different substituents and aldol additions of α-substituted glycolic acid derivatives.1 Introduction1.1 Organization of this Review1.2 Outside the Scope of this Review: Aldol Additions Giving α,β-Dihydroxyaldehydes and α,β-Dihydroxyketones Diastereoselectively1.3 Non-Aldol Routes to Diastereomerically Pure α,β-Dihydroxycarboxylic Acid Derivatives2 Aldol Additions of Glycolic Acid (Derivative) Enolates to Aldehydes2.1 Aldol Additions of Glycolate Enolates (‘Glycolic Acid Dianions’)2.2 Aldol Additions of Glycolic Ester Enolates2.3 Aldol Additions of Glycolic Thioester Enolates2.4 Aldol Additions of Glycolimide Enolates2.5 Aldol Additions of Glycolamide Enolates2.6 Mukaiyama Aldol Additions of Silyl Ketene Acetals of Glycolic Esters and Thioesters2.7 Aldol Additions of Glycoloyl Chlorides via Acyl Ammonium Enolates3 Aldol-Providing Substitutions of Glycolimide Enolates in Acetals4 Additions Related to Aldol Additions of Glycolic Acid Derivative Enolates to Aldehydes4.1 Selected Simply Diastereoselective Aldol Additions of Enolates of Glycolic Acid Derivatives to Ketones with Two Different Substituents4.2 Simply Diastereoselective Aldol Additions of Enolates of Glycolic Acid Derivatives with a Methyl Substituent at C-α (Lactic Acid Derivatives)5 Conclusion

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Holý, Antonín, Joachim König, Jiří Veselý, Dieter Cech, Ivan Votruba, and Erik De Clercq. "5'-O-Alkyl-5-fluorouridines: Synthesis and biological activity." Collection of Czechoslovak Chemical Communications 52, no. 6 (1987): 1589–608. http://dx.doi.org/10.1135/cccc19871589.

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Methyl 2,3-O-isopropylidene-D-ribofuranoside (IV) was alkylated with alkyl halides in the presence of sodium hydride and the products were transformed by acid hydrolysis and glycosylation into methyl 5-O-alkyl-D-ribofuranosides VII. Benzoylation of VII followed by acetolysis afforded 1-O-acetyl-2,3-di-O-benzoyl-5-O-alkyl-D-ribofuranoses IX which on reaction with 2,4-bis(trimethylsilyloxy)pyrimidine in the presence of tin tetrachloride in acetonitrile and subsequent hydrolysis gave 5'-O-alkyl-2',3'-di-O-benzoyluridines XIa-XIe. Methanolysis of compounds XI furnished 5'-O-alkyluridines III. The 5-O-allyl derivative XII was hydroxylated in the presence OsO4 and transformed further to 5'-O-(RS)-(2,3-dihydroxypropyl)uridine (IIIg) and its tetrabenzoate XVI. Compounds XI and XVI on reaction with elemental fluorine in acetic acid afforded benzoyl derivatives of 5'-O-alkyl-5-fluorouridines XVIIa-XVIIe and XIX which were methanolyzed to give 5'-O-alkyl-5-fluorouridines II. This procedure afforded 5'-O-methyl (IIa), ethyl (IIb), n-butyl (IIc), n-hexyl (IId), n-octyl (IIe), and (RS)-(2,3-dihydroxypropyl) (IIf) derivatives of 5-fluorouridine. None of the compounds II exhibited antibacterial effect on Escherichia coli B or antiviral activity against HSV-1, HSV-2, vaccinia virus or vesicular stomatitis viruses. Compounds IIc,d,e suppressed the growth of L 1210 mice leukemic cells at concentrations of 10-5 to 10-6 mol l-1; the 5'-O-n-butyl derivative IIc has the highest activity (ID50 2·8 μmol l-1) but does not prolong the life span of L 1210 leukemia bearing mice following repeated daily doses of 80 mg/kg.

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Mistry, Rakesh N., and K. R. Desai. "Studies on Synthesis of Some Novel Heterocyclic Azlactone Derivatives and Imidazolinone Derivatives and their Antimicrobial Activity." E-Journal of Chemistry 2, no. 1 (2005): 42–51. http://dx.doi.org/10.1155/2005/542938.

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p- Methyl benzoic acid on reaction with phosphorus pentachloride gives p - methyl benzoyl chloride derivative which on condensation with glycine gives p - methyl benzoyl glycine derivative. Now, this p - methyl benzoyl glycine derivative on condensation with various substituted aldehydes gives corresponding substituted 4 - [aryl methylidine] - 2 - [p - methyl phenyl] - oxazole - 5 - one derivatives [1(a-j)]. Further, these derivatives [1(a-j)] on condensation with 4 , 4’ - diamino diphenyl sulphone gives corresponding substituted imidazolinone - dibenzsulphone derivatives [2(a-j)], on condensation with 4 , 4’ - diamino diphenyl methane gives corresponding substituted imidazolinone - dibenzmethane derivatives [3(a-j)], on condensation with 4,4’- diamino benzanilide gives corresponding substituted imidazolinone - benzanilide derivatives [4(a-j)] and on condensation with 2 - amino pyridine gives corresponding substituted imidazolinone - pyridine derivatives [5(a-j)] respectively. Structure elucidation of synthesised compounds has been made on the basis of elemental analysis, I.R. spectral studies and1H N.M.R. spectral studies. The antimicrobial activity of the synthesised compounds has been studied against the cultures “Staphylococcus aureus”, “Escherichia coli” and “Candela albicans”.

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10

Dutta, Saikat, Linglin Wu, and Mark Mascal. "Production of 5-(chloromethyl)furan-2-carbonyl chloride and furan-2,5-dicarbonyl chloride from biomass-derived 5-(chloromethyl)furfural (CMF)." Green Chemistry 17, no. 7 (2015): 3737–39. http://dx.doi.org/10.1039/c5gc00936g.

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Biomass-derived CMF is oxidized to the acid chloride CMFCC in a single step using inexpensive t-butyl hypochlorite. Likewise, DFF, also a CMF derivative, is oxidized directly to the diacid chloride FDCC. The products are platforms for a variety of chemical derivatives of carbohydrates.

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11

Panyatip, Panyada, Nadtanet Nunthaboot, and Ploenthip Puthongking. "In Silico ADME, Metabolism Prediction and Hydrolysis Study of Melatonin Derivatives." International Journal of Tryptophan Research 13 (January 2020): 117864692097824. http://dx.doi.org/10.1177/1178646920978245.

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Melatonin (MLT) is a well-known pineal hormone possessed with remarkable biological activities. However, its low oral bioavailability and high first-pass metabolism rate are important pharmacokinetics problems. Therefore, 5 MLT derivatives (1-5) were designed and synthesised in our group to solve these problems. In this work, in silico analysis of all synthetic derivatives for pharmacokinetic and drug-likeness parameters were predicted by SwissADME software. The results revealed that all derivatives (1-5) met the requirements for ideal oral bioavailability and CNS drugs. The molecular docking showed that the acetyl-MLT derivative (1) and the un-substitution at N1-position derivative 5 would be substrates of CYP1A2, while the lipophilic substituted N1-position derivatives 2-4 could not be metabolised by CYP1A2. Moreover, all N-amide derivatives (1-4) were hydrolysed and released less than 2.33% MLT after 4-hour incubation in 80% human plasma. It seemed that these derivatives preferred to behave like drugs rather than prodrugs of MLT. These findings confirmed that the addition of bulky groups at the N1-position of the MLT core could prolong the half-life, increase drug absorption and penetrate the blood brain barrier into the CNS.

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Abdelhamid, Abdou Osman, and A. S. Shawali. "Synthesis of Some New 2-Imino-2,3-dihydro-1,3,4-thiadiazole and Selenadiazole Derivatives." Zeitschrift für Naturforschung B 42, no. 5 (1987): 613–16. http://dx.doi.org/10.1515/znb-1987-0516.

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(2)Diazotized 3(5)amino-5(3)-phenylpyrazole reacts with phenacylthiocyanate (1) and phenacylselenocyanate (10) to give the corresponding 1,3,4-thiadiazoline derivative (5) and 1,3,4- selenadiazoline derivative (12), respectively. A mechanism is proposed and it is substantiated by an alternate synthesis of 5 and 12 from the corresponding hydrazidoyl bromide (6) with potassium thiocyanate and potassium selenocyanate, respectively. The thiadiazoline (5) and selenadiazoline (12) give the respective N-acyl derivatives (7a) and (12) with acetic anhydride. Nitrosation of 5 and 12 gives the corresponding N-nitroso-derivatives (8a) and (14), respectively. Cyclization of 6 gives the corresponding 9 with triethylamine in benzene.

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13

Zhou, Qishun, Bao Vu Ngoc, Grazyna Leszczynska, Jean-Luc Stigliani, and Geneviève Pratviel. "Oxidation of 5-methylaminomethyl uridine (mnm5U) by Oxone Leads to Aldonitrone Derivatives." Biomolecules 8, no. 4 (2018): 145. http://dx.doi.org/10.3390/biom8040145.

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Oxidative RNA damage is linked to cell dysfunction and diseases. The present work focuses on the in vitro oxidation of 5-methylaminomethyl uridine (mnm5U), which belongs to the numerous post-transcriptional modifications that are found in tRNA. The reaction of oxone with mnm5U in water at pH 7.5 leads to two aldonitrone derivatives. They form by two oxidation steps and one dehydration step. Therefore, the potential oxidation products of mnm5U in vivo may not be only aldonitrones, but also hydroxylamine and imine derivatives (which may be chemically more reactive). Irradiation of aldonitrone leads to unstable oxaziridine derivatives that are susceptible to isomerization to amide or to hydrolysis to aldehyde derivative.

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14

Welchinskaya, Elena. "CHEMISTRY AND ANTITUMOUR ACTIVITY OF 5-BROMOURACILE’S DERIVATIVES." CBU International Conference Proceedings 1 (June 30, 2013): 279–85. http://dx.doi.org/10.12955/cbup.v1.45.

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Problemofthetreatmentof man’scancerandsearchoftheeffective, withalittletoxicityantitumourmedicalproducts,isonefromtheimportant taskatthecontemporaneous medicine and pharmaceutical chemistry. Chemicalmodificationofmolecularof5-bromouracilewithnextinvestigationoftoxicity and antitumour activityofits newderivativeswhichsynthesized is described. Physical-chemical, statistical pharmacological, toxicological methods were used. A strongly antitumour effect has been discovered for bis-derivative of 5-bromouracile for the first time. A new convenient methods for the preparation of new mono- and bis-derivatives of 5-bromouracile with 1,1,1-trifluoro-2-bromo-2-chloroethane (ftorotan) and 1,1-diethylcarboxy-2-chloro-2-trifluoromethylethylene is described. The reactions are catalyzed by the DB-18-crown-6-complex. It was tested on the heterotransplantates of man’s glioma cancer of brain (by Bogden’s under capsule-method). It is permits to consider the new bis-derivative of 5-bromouracile as physiological active with a perspective investigation as potential antitumour drugs for treatment of man in future.

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15

Khan, Khurshid Alam, M. Qudrat-e-Khuda, and Viqar Uddin Ahmad. "Studies on the Alkylation of 5′-CMP under Alkaline Conditions." Zeitschrift für Naturforschung B 47, no. 9 (1992): 1307–13. http://dx.doi.org/10.1515/znb-1992-0916.

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The reaction of 5′-CMP with methyl, ethyl, n-propyl and isopropyl iodides gave predominantly ribose alkylated products. Various alkylated derivatives have been characterized using UV spectroscopy, paper electrophoresis, 1H NMR and FAB (negative) mass spectroscopic techniques. Under strongly alkaline conditions the 2′-O-alkylated derivatives are synthesized in maximal yields. Isopropylation reaction gave only a small yield of the 3′-O-isopropyl derivative, this could be explained on the basis of steric hindrance offered to the bulky isopropyl group at the 2′-OH position by the heterocyclic base of the nucleotide.

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16

Konečný, Václav, Jozefína Žúžiová, Štefan Kováč, and Tibor Liptaj. "Synthesis of Novel 4-Amino-5-(disubstituted amino)-2-phenyl-2H-pyridazin-3-ones." Collection of Czechoslovak Chemical Communications 62, no. 5 (1997): 800–808. http://dx.doi.org/10.1135/cccc19970800.

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Substituted 4-amino-2-phenyl-2H-pyridazin-3-ones 5a-5j have been prepared from 4-amino-5-chloro-2-phenyl-2H-pyridazin-3-one 1 which on reactions with acetyl chloride or acetic anhydride gives 4-acetylamino derivative 2 or 4-diacetylamino derivative 3, respectively. Derivatives 2 and 3 with dialkylamines and cyclic amines yielded appropriate 4-acetylamino-5-(disubstituted amino)-2-phenyl-2H-pyridazin-3-ones 4a-4j. Subsequent alkaline hydrolysis of the acetylamino derivatives 4a-4j let to the title compounds 5a-5j, which were screened for pesticidal activity, but none of them reached activity of the used standards.

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17

Brualdi, Richard A., and Geir Dahl. "Permutation Matrices, Their Discrete Derivatives and Extremal Properties." Vietnam Journal of Mathematics 48, no. 4 (2020): 719–40. http://dx.doi.org/10.1007/s10013-020-00392-5.

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AbstractFor a permutation π, and the corresponding permutation matrix, we introduce the notion of discrete derivative, obtained by taking differences of successive entries in π. We characterize the possible derivatives of permutations, and consider questions for permutations with certain properties satisfied by the derivative. For instance, we consider permutations with distinct derivatives, and the relationship to so-called Costas arrays.

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Nazarova, Anastasia, Pavel Padnya, Arthur Khannanov, Aleksandra Khabibrakhmanova, Pavel Zelenikhin, and Ivan Stoikov. "Towards Protection of Nucleic Acids from Herbicide Attack: Self-Assembly of Betaines Based on Pillar[5]arene with Glyphosate and DNA." International Journal of Molecular Sciences 24, no. 9 (2023): 8357. http://dx.doi.org/10.3390/ijms24098357.

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Herbicides are one of the main parts of pesticides used today. Due to the high efficiency and widespread use of glyphosate-based herbicides, the search for substances reducing their genotoxicity is an important interdisciplinary task. One possible approach for solving the problem of herbicide toxicity is to use compounds that can protect DNA from damage by glyphosate derivatives. For the first time, a method for developing DNA-protecting measures against glyphosate isopropylamine salt (GIS) damage was presented and realized, based on low-toxicity water-soluble pillar[5]arene derivatives. Two- and three-component systems based on pillar[5]arene derivatives, GIS, and model DNA from salmon sperm, as well as their cytotoxicity, were studied. The synthesized pillar[5]arene derivatives do not interact with GIS, while GIS is able to bind DNA from salmon sperm with lgKa = 4.92. The pillar[5]arene betaine derivative containing fragments of L-phenylalanine and the ester derivative with diglycine fragments bind DNA with lgKa = 5.24 and lgKa = 4.88, respectively. The study of the associates (pillar[5]arene-DNA) with GIS showed that the interaction of GIS with DNA is inhibited only by the betaine pillar[5]arene containing fragments of L-Phe (lgKa = 3.60). This study has shown a possible application of betaine pillar[5]arene derivatives for nucleic acid protection according to its competitive binding with biomacromolecules.

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Machida, H., S. Sakata, N. Ashida, K. Takenuki, and A. Matsuda. "In vitro Anti-Herpesvirus Activities of 5-Substituted 2′-Deoxy-2′-Methylidene Pyrimidine Nucleosides." Antiviral Chemistry and Chemotherapy 4, no. 1 (1993): 11–17. http://dx.doi.org/10.1177/095632029300400102.

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New pyrimidine deoxyribonucleoside analogues, 2′-deoxy-2′-methylideneuridine (DMDU), 2′-deoxy-2′-methylidenecytidine (DMDC), and their 5-substituted derivatives were tested for the anti-herpesvirus activities and anti-proliferative activity. E-5-(2-Bromovinyl)uracil derivative (BV-DMDU) and its cytosine congener were synthesized from 1-β-D-arabinofuranosyl- E-5-(2-bromovinyl)uracil (BV-araU). 5-Bromo, 5-iodo, 5-methyl, and 5-ethyl derivatives of DMDU and BV-DMDU showed activities against herpes simplex virus type 1 (HSV-1) and varicella-zoster virus (VZV). The corresponding DMDC derivatives had no or only weak antiviral activity. Among the 2′-deoxy-2′-methylidene pyrimidine nucleosides, BV-DMDU showed the most potent and selective anti-VZV activity. BV-DMDU was more potent than acyclovir, but less active than BV-araU. BV-DMDU was inactive against human diploid and tumour cells. DMDC and F-DMDC (5-fluoro derivative) were potent inhibitors of HSV-1, herpes simplex virus type 2, VZV, and human cytomegalovirus (HCMV) and also had significant anti-proliferative activity. Their potency against HCMV was better than that of ganciclovir and araC. Some DMDU derivatives also showed anti-HCMV activity, but they had anti-proliferative activity. The anti-HCMV activity of these DMDC and DMDU compounds was generally more potent than those against HSV-1 and VZV thereof, suggesting the participation of cellular kinase in their antiviral action.

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Werfeli, Ali, Svatava Voltrová, Viktor Prutianov, and Josef Kuthan. "Optically Active Furanoids Containing Cytosine-, Adenine- and Nicotinamide-Like Moieties." Collection of Czechoslovak Chemical Communications 61, no. 8 (1996): 1223–32. http://dx.doi.org/10.1135/cccc19961223.

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3-Hydroxymethyl-5-(2,3-O-isopropylidene-β-D-erythro-furanosyl)-2-methylfuran (2) prepared from 3-ethoxycarbonyl derivative 1 was converted to 3-chloromethyl-5-(2,3-O-isopropylidene-β-D-erythro-furanosyl)-2-methylfuran (3). Compound 3 reacted with cytosine, adenine, 6-chloropurine, 6-mercaptopurine, and nicotinamide to corresponding optically active heterocyclic derivatives 5-10 and 14. The 6-chloro derivative 9 was converted to 6-alkoxy derivatives 11 and 12 by the reaction with methanol or ethanol, respectively, in the presence of diazabicyclooctane. Dithionite reduction of quaternary chloride 14 gave 1,4-dihydropyridine derivative 15 capable to transform ethyl phenylglyoxylate to optically active ethyl mandelate.

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21

Ruissen, A. L. A., J. Groenink, W. Van ’t Hof, et al. "Histatin 5 and derivatives." Peptides 23, no. 8 (2002): 1391–99. http://dx.doi.org/10.1016/s0196-9781(02)00076-1.

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22

Zhong, Yi Ping, Xue Quan Zhao, Li Guan, Ping Liu, and Wen Ji Deng. "Preparation and Electrochromic Properties of Polythiophene Derivatives." Key Engineering Materials 538 (January 2013): 7–10. http://dx.doi.org/10.4028/www.scientific.net/kem.538.7.

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Polythiophene derivatives, poly(2,2′:5′,2″:5″,2″′:5″′,2″″-quinquethiophene) (P5T), poly (2,3,4,5-tetrathiopenyl-thiophene) (PX5T) and poly(1,3,5-tristhienyl-benzene) (P3TB), were prepared via the electropolymerization. The electrochromic properties of polythiophene derivative films were investigated. The results showed that P5T, PX5T and P3TB films exhibited reversible, clear colour change in liquid electrolyte on electrochemical doping and dedoping. Moreover, solid state electrochromic device, indium tin oxide (ITO)/polythiophene derivative films/conducting gel /ITO, were fabricated with polythiophene derivative films as the active electrochromic layer. The color change of polythiophene derivative films based on gel electrolyte on electrochemical doping and dedoping were similar with the color change based on liquid electrolyte.

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23

Liepa, AJ, AJ Liepa, JS Wilkie, JS Wilkie, KN Winzenberg, and KN Winzenberg. "Preparation of Some 1-Alkyl-4-[1-(ethoxyimino)butyl]-3-hydroxy-5-oxocyclohex-3-ene-1-carboxylic Acid Ester and Amide Herbicides by Reductive Alkylation of 3,5-Dimethoxybenzoic Acid." Australian Journal of Chemistry 42, no. 8 (1989): 1217. http://dx.doi.org/10.1071/ch9891217.

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Reductive alkylation of 3,5-dimethoxybenzoic acid with haloalkanes afforded the 1-alkyl- 3,5-dimethoxycyclohexa-2,5-diene-1-carboxylic acid derivatives (3a-e) which, upon esterification and hydrolysis, furnished methyl 1-alkyl-3-hydroxy-5-oxocyclohex-3-ene-l-carboxylate derivatives (4f-j). Reaction of (4f-j) with butyric anhydride gave methyl 1-alkyl-4-butyryl- 3-hydroxy-5-oxocyclohex-3-ene-1-carboxylate derivatives (6a-e) which were converted into methyl 1-alkyl-4-[1-( ethoxyimino )butyl]-3-hydroxy-5-oxocyclohex-3-ene-1-carbo xyate derivatives (2a-e). Similarly, the oxime O-ether derivative (2f) was prepared from the amide (41), obtained from reaction of (3b) with N,N′- carbonyldiimidazole and dimethylamine followed by hydrolysis.

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24

Iwamoto, Shintaro, Yuu Inatomi, Daisuke Ogi, et al. "New tris- and pentakis-fused donors containing extended tetrathiafulvalenes: New positive electrode materials for rechargeable batteries." Beilstein Journal of Organic Chemistry 11 (July 8, 2015): 1136–47. http://dx.doi.org/10.3762/bjoc.11.128.

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Derivatives of tris-fused TTF extended with two ethanediylidenes (5), tris- and pentakis-fused TTFs extended with two thiophene-2,5-diylidenes (6–9) were successfully synthesized. Cyclic voltammograms of the tetrakis(n-hexylthio) derivative of 5 and 7 (5d, 7d) consisted of two pairs of two-electron redox waves and two pairs of one-electron redox waves. On the other hand, four pairs of two-electron redox waves and two pairs of one-electron redox waves were observed for the tetrakis(n-hexylthio) derivative of 9 (9d). Coin-type cells using the bis(ethylenedithio) derivatives of 5 (5b), 6 (6b) and the tetrakis(methylthio) derivatives of 5 (5c) and 8 (8c) as positive electrode materials showed initial discharge capacities of 157–190 mAh g−1 and initial energy densities of 535–680 mAh g−1. The discharge capacities after 40 cycles were 64–86% of the initial discharge capacities.

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25

Khalifa, Nagy M., Ahmed M. Naglah, Mohamed A. Al-Omara, and Abd El-Galil E. Amr. "Synthesis and Reactions of New Chiral Linear Dipeptide Candidates Using Nalidixic Acid as Starting Material." Zeitschrift für Naturforschung B 69, no. 6 (2014): 728–36. http://dx.doi.org/10.5560/znb.2014-4031.

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A series of dipeptide heterocyclic derivatives 4-15 were synthesized using methyl 2-{[(1-ethyl- 7-methyl-4-oxo-1,4-dihydro-1,8-naphthyridin-3-yl)carbonyl]amino}-3-ethylbutanoate (3) as starting material. Treatment of 3 with L-phenylalanine methyl ester hydrochloride afforded the corresponding dipeptide methyl ester derivative 4, which was treated with hydrazine hydrate to afford the dipeptide acid hydrazide 5. Compound 5 was coupled with aldehyde and acetophenone derivatives to afford the corresponding Schiff bases 6a-f. The hydrazide derivative 5 was reacted with ethyl acetoacetate or acetone to give compounds 7 and 8, respectively. Reaction of 5 with carbon disulfide at different conditions afforded compounds 9 and 10, which were treated with hydrazine hydrate to give the 1-amino-2-dipeptido-1,3,4-triazole derivative 11. In addition, 5 was reacted with phenyl isothiocyanate to give the thiosemicarbazide derivative 12, which was cyclized with sodium hydroxide to the dipeptido 1-phenyl-1,3,4-triazole derivative 13. Finally, treatment of 13 with methyl iodide afforded the S-methyl derivative 14, which was reacted with hydrazine hydrate to give the hydrazine derivative 15.

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26

Harnden, MR, and DT Hurst. "The Chemistry of Pyrimidinethiols. III. The Synthesis of Some Substituted Pyrimidinthiols and Some Thiazolo[5,4-D]pyrimidines." Australian Journal of Chemistry 43, no. 1 (1990): 55. http://dx.doi.org/10.1071/ch9900055.

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The preparation of a number of pyrimidinethiols and (substituted) thiopyrimidines has been carried out. The reaction of 5-acetylamino-2-aminopyrimidine-4,6-diol with phosphorus penta -sulfide in pyridine gave 5-amino-2-methylthiazolo[5,4-d]pyrimidine-7-thiol which was used to prepare several additional novel pyrimidine derivatives. Hydrolysis of the 4-carboxymethylthio derivative by using 5M hydrochloric acid gave 2,5-diamino-6-mercaptopyrimidin-4-ol hy -drochloride whilst hydrolysis of 2-methyl-7-methylthiothiazolo[5,4-d]pyrimidin-5-amine gave the corresponding 4-hydroxy derivative. Several 4-arenecarbonylmethylthio derivatives were recovered unchanged from such hydrolysis reactions.

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27

Černý, Ivan, Vladimír Pouzar, Miloš Buděšínský, Pavel Drašar та Miroslav Havel. "Epimeric 17-hydroxy derivatives of 14β-androst-5-en-3β-yl acetate". Collection of Czechoslovak Chemical Communications 55, № 10 (1990): 2510–20. http://dx.doi.org/10.1135/cccc19902510.

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A new, six-step synthesis of 3β-hydroxy-14β-androst-5-en-17-one (IX) starting from 3β-hydroxyandrost-5-en-17-one has been elaborated. Reduction of acetate X with sodium borohydride afforded 17α-hydroxy-14β-androst-5-en-3β-yl acetate (XI). The corresponding 17β-derivative XIV was obtained by epimerization of 17α-O-tosyl derivative XIII with sodium nitrite in hexamethylphosphoramide. The 13C and 1H NMR spectra of 14β-androstane derivatives are discussed.

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28

Asma, Noor. "In-silico analysis of tenidap and its derivative as a novel 5-lipoxygenase inhibitor." International Journal of Pharmaceutical Sciences and Developmental Research 3, no. 1 (2018): 036–38. https://doi.org/10.17352/ijpsdr.000015.

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Tenidap is a derivative of Flavonoids which are actually plant derivatives, it shows inhibition activity of 5-lipoxygenase. Molecular models were directed to discover molecular docking mode, also to help explain molecular tool behind its inhibitory action. Molecular relations of tenidap with the catalytic trio (His523, His518, Ile875) inside active or dynamic position of 5-lipoxygenase through hydrogen bonding, appears to the major reason elaborate in its substantial 5-lipoxygenase activity of inhibition.

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29

Al-Harbi, Reem A. K. "Synthesis of New Coumarin Scaffold Bearing 2-Iminochromene Moiety." Acta Chimica Slovenica 70, no. 3 (2023): 380–84. http://dx.doi.org/10.17344/acsi.2023.8016.

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Coumarin is classified as one of interesting therapeutic starting research points to obtain remarkable compounds with high efficacy. So, during this research, new 2-iminochromene derivatives bearing coumarin moiety were synthesized. At first, cyanoacetohydrazone of 3-acetylcoumarin was prepared and used as the starting material. The 2-iminochromene derivatives were synthesized through the ring closure of cyanoacetohydrazone derivative with 4-hydroxysalicylaldehyde, 5-aryldiazosalicylaldehydes, 2-hydroxynaphthaldehyde and 7-hydroxychromone-6-carboxaldehyde derivative. All of the newly synthesized coumarin derivatives were obtained in excellent yields; so, the new synthesized coumarin derivatives will participate in the enrichment of the chemical libraries.

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30

Thanki, Pragna H., Dhaval V. Hingrajiya, Jayesh J. Modha, and Jalpa H. Vadgama. "Synthesis, characterization and antibiotic evaluation of various biologically active derivatives of 4-Alkylpyrimidine-5-carbonitrile." Current Chemistry Letters 12, no. 3 (2023): 537–44. http://dx.doi.org/10.5267/j.ccl.2023.3.002.

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Extensive research work has been published on Tetrahydro and Dihydropyrimidine derivatives. Pyrimidine-5-Carbonitrile and its analogs have demonstrated a large number of activities. Some 6-Halogenosubstituted pyrimidine analogs have also been reported to be biologically active to a certain extent, but the literature survey reveals not much report on 6-alkylated pyrimidine derivatives. Targeting enhancement in biologically useful properties of a lead molecule through the association of it with active pharmacophoric groups or molecules is a conventional method in pharmaceutical research. With an aim to explore a better useful Dihydropyrimidine derivative, a newer 4-Alkylated-1,6-dihydropyrimidine analog (1) has been prepared. The lead molecule (1) has further been converted to amine derivative (2), hydrazino derivative (3) tri substituted s-triazinyl derivative (4), sulphonamide (5), Schiff’s base (6), a thiazolidinones (7), and 2-Azetidinones (8) respectively using various methods. Compounds 2, 4, 5, and 7 showed 50% and 8 showed 100% bacterial inhibition at 32μg/mL in single-point bacterial inhibition against various bacterial strains.

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31

Bedair, A. H., Abd El-Wahab, A. M. El-Agrody, F. M. Ali, A. H. Halawa, and G. M. El-Sherbiny. "Binary heterocyclic systems containing the ethylideneamino linkage: synthesis of some new heterocyclic compounds bearing the naphtho-[2,1-b]furan moiety." Journal of the Serbian Chemical Society 71, no. 5 (2006): 459–69. http://dx.doi.org/10.2298/jsc0605459b.

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Ethylidene hydrazine (4a,b) and thiazolidin-4-one (5) derivatives were synthesized by the reaction of ethylidenethiosemicarbazide derivative (3a) with ?-haloketone/ethyl bromoacetate, respectively. Hetrocyclization of ethylideneacetohydrazide derivative (7) with o-phenolic aldehydes gave the corresponding coumarin derivatives (8,9). The interaction of 7 with acetylacetone afforded the corresponding pyridine derivative (10). Treatment of the arylidene derivative 11b with malononitrile afforded the corresponding pyran derivative (12). The new products 3-12 were subjected to IR, 1H NMR and mass spectra studies.

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32

Ahmed, Naglaa M., Ahmed H. Lotfallah, Mohamed S. Gaballah, Samir M. Awad, and Moustafa K. Soltan. "Novel 2-Thiouracil-5-Sulfonamide Derivatives: Design, Synthesis, Molecular Docking, and Biological Evaluation as Antioxidants with 15-LOX Inhibition." Molecules 28, no. 4 (2023): 1925. http://dx.doi.org/10.3390/molecules28041925.

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New antioxidant agents are urgently required to combat oxidative stress, which is linked to the emergence of serious diseases. In an effort to discover potent antioxidant agents, a novel series of 2-thiouracil-5-sulfonamides (4–9) were designed and synthesized. In line with this approach, our target new compounds were prepared from methyl ketone derivative 3, which was used as a blocking unit for further synthesis of a novel series of chalcone derivatives 4a–d, thiosemicarbazone derivatives 5a–d, pyridine derivatives 6a–d and 7a–d, bromo acetyl derivative 8, and thiazole derivatives 9a–d. All compounds were evaluated as antioxidants against 2,2-diphenyl-1-picrylhydrazyl (DPPH), hydrogen peroxide (H2O2), lipid peroxidation, and 15-lipoxygenase (15-LOX) inhibition activity. Compounds 5c, 6d, 7d, 9b, 9c, and 9d demonstrated significant RSA in all three techniques in comparison with ascorbic acid and 15-LOX inhibitory effectiveness using quercetin as a standard. Molecular docking of compound 9b endorsed its proper binding at the active site pocket of the human 15-LOX which explains its potent antioxidant activity in comparison with standard ascorbic acid.

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33

Vadla, Balakishan, Naveen Puram, and Sailu Betala. "Novel trifluoromethyl-thieno[2,3-b]pyridine-2-carboxamide and Schiff’s base derivatives and their anticancer activity." Research Journal of Chemistry and Environment 27`, no. 9 (2023): 69–74. http://dx.doi.org/10.25303/2709rjce069074.

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A series of novel trifluoromethyl-thieno[2,3-b] pyridine-2-carboxamide 3a-h and Schiff’s base derivatives 5a-g was prepared starting from 6-methyl-2-oxo-4-(trifluoromethyl)-1,2-dihydropyridine-3-carb onitrile 1. Compound 1 on reaction with bromoethyl acetate produced ester derivative 2 on reaction with different amines produced amide derivatives 3. Ester derivative 2 which on reaction with hydrazine hydrate gave hydrazide 4 derivative. Further this compound on reaction with different substituted aromatic aldehydes formed Schiff’s base derivatives 5. All the products 3a-h and 5a-f were screened against four human cancer cell lines such as HeLa -Cervical cancer (CCL-2), COLO 205-Colon cancer (CCL-222), HepG2-Liver cancer (HB-8065) and MCF7-Breast cancer (HTB-22). Promising compounds 3a and 3c have been identified with reference to standard control of 5-Fluorouracil.

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34

Al-Ghamdi, Youssef O., Khalid A. Alamry, Mahmoud A. Hussein, Hadi M. Marwani, and Abdullah M. Asiri. "Sulfone-modified chitosan as selective adsorbent for the extraction of toxic Hg(II) metal ions." Adsorption Science & Technology 37, no. 1-2 (2018): 139–59. http://dx.doi.org/10.1177/0263617418818957.

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In this study, a new category of sulfone-modified chitosan derivatives as surface-selective adsorbents for the extraction of toxic Hg(II) metal has been synthesized in good yield. Sulfone-modified chitosan/5–20 based on variable loading of the corresponding phenacyl bromide (5, 10, 15, and 20% with respect to the original weight of the pure chitosan) was synthesized. The β-ketosulfone derivative, namely 1–(4-bromophenyl)-2-(phenylsulfonyl)ethanone, was first prepared by treatment of the corresponding phenacyl bromide with a sufficient amount of sodium benzene sulfinate; its chemical structure was confirmed by spectral analyses, including Fourier transform infrared spectroscopy, 1H-NMR, 13C-NMR, and mass spectrometry. Then, sulfone-modified chitosan/5–20 derivatives were synthesized by the interaction of chitosan with a freshly prepared p-bromo-β-ketosulfone derivative in a mildly acidic aqueous solution using the solution-blending technique. Sulfone-modified chitosan/5–20 derivatives were identified and characterized using common characterization techniques, including Fourier transform infrared spectroscopy, ﬁeld-emission scanning electron microscope, powder X-ray diffraction, and thermal behaviour. A strong interaction was displayed between chitosan and its corresponding β-ketosulfones in powder X-ray diffraction, which was confirmed by significant 2θ shifts. Sulfone-modified chitosan/5–20 derivatives were detected as catalysts, which efficiently increased the thermal decomposition of pure chitosan. More particularly, the efficiency of sulfone-modified chitosan/5–20 derivatives for Hg(II), Pb(II), Ni(II), Al(III), Sr(II), Cr(III), Fe(III), Zn(II), and Mn(II) detection and adsorption was also investigated using inductively coupled plasma optical emission spectrometry. The sulfone-modified chitosan/5 derivative exhibited the highest adsorption efficiency. The most effective quantitative adsorption onto the sulfone-modified chitosan/5 surface was detected at pH = 2. In addition to that, the adsorption isotherm showed that the adsorption capacity of sulfone-modified chitosan/5 for Hg(II) was 122.47 mg g−1 and that its adsorption isotherm was in agreement with the Langmuir adsorption isotherm.

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35

Ammar Ferman Abbood, Ahmed M. Abdula, and Younis Baqi. "New Benzimidazoles Bearin 2-Pyrazoline Moiety: Synthesis and Antimicrobial Activity." Journal of Wasit for Science and Medicine 14, no. 3 (2023): 1–12. http://dx.doi.org/10.31185/jwsm.401.

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A new series of 5-(1H-Benzimidazol-2-yl)-4,5-dihydro-1H-pyrazol-3-yl] derivatives (1-9) were synthesized and characterized using spectral analysis. The first step includes the reaction of benzimidazole-2-carboxaldehyde with the o,p-aminoacetophenone to obtain the chalcone derivative (1, 2). The cyclization reaction of chalcone by the hydrazine hydrate afforded compound (3, 4), which represents the starting material for Schiff base derivatives. New Schiff bases (5-6) were synthesized from the reaction of benzimidazole derivative (2) with the corresponding benzaldehydes. The azetidin-2-one (7) and 1,3-oxazepane-4,7-dione derivatives (8-9) were synthesized from the corresponding aldehyde with chloroacetyl chloride and appropriate anhydride as depicted in the experimental section. All the derivatives were in vitro screened against Escherichia coli, Klebsiella spp. (Gram negative), Staphylococcus aureus, S.espidermi (Gram positive) as well as Candida albicans and found to exhibit moderate to potent activity.

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36

Abdel-Rahman, Adel A. H., and Takeshi Wada. "Synthesis and Antiviral Evaluation of 5-(1,2,3-Triazol-1-ylmethyl)- uridine Derivatives." Zeitschrift für Naturforschung C 64, no. 3-4 (2009): 163–66. http://dx.doi.org/10.1515/znc-2009-3-402.

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Some 5-(1,2,3-triazol-1-ylmethyl)uridine derivatives were synthesized via the 1,3-dipolar cycloaddition of a 5-azidomethyluridine derivative with substituted acetylenes. The antiviral activities of these compounds against hepatitis A virus (HAV, MBB cell culture-adapted strain) and Herpes simplex virus type-1 (HSV-1) were tested.

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37

Gakovic, Andrea, Maja Djurendic-Brenesel, Evgenija Djurendic, Katarina Penov-Gasi, and Marija Sakac. "Synthesis of some 16,17-secoandrost-5-ene derivatives." Chemical Industry 64, no. 2 (2010): 81–84. http://dx.doi.org/10.2298/hemind100212009g.

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Starting from 3?-acetoxy-17-oxo-16,17-secoandrost-5-ene-16-nitrile (1), 3?-acetoxy-16,17-secoandrost-5-ene-16-nitrile (4) was synthesized by a three-stage procedure. First, the formyl group of compound 1 was reduced, to yield the alcohol 2. Compound 2 was further transformed to the mesyloxy derivative 3, whose reduction with NaBH3CN gave compound 4. Apart from compound 4 as the main reaction product, two additional products were obtained, for which the GC/MS analysis suggested that they are 8(14) and 14 derivatives of compound 4. Compound 4 was transformed into 3?-hydroxy-16,17-sesoandrost-5-ene-16-nitrile (7), the Oppenauer oxidation of which afforded 3-oxo-16,17-secoandrost-4-ene-16-nitrile (8).

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38

Holman, Glen, Carlos Correia, Lucian Pitt, and Akios Majoni. "The corporate use of derivatives by listed non-financial firms in Africa." Corporate Ownership and Control 11, no. 1 (2013): 671–90. http://dx.doi.org/10.22495/cocv11i1c7art5.

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This paper presents the results of an extensive analysis of derivative use by 692 companies in 20 countries across the African continent. The results show that 29% of non-financial companies in Africa use derivatives but that derivative use is dominated by firms within South Africa. The study finds that 54% of firms in South Africa use derivatives but only 5% of non-financial firms in Africa (excluding South Africa) use derivatives for hedging purposes. The majority of derivative use is directed toward the management of currency risks and the derivative instrument of choice is OTC forwards. Swaps are used to hedge interest rate risk and minimal use is made of OTC or exchange traded options and futures

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39

Wang, Jin, Teng-huo-sheng Liao, and Jian Yang. "Efficient synthesis of 2,3-dimethoxy-5-methyl-6-morpholinomethyl-1,4-benzoquinone hydrochloride." Zeitschrift für Naturforschung B 70, no. 4 (2015): 221–23. http://dx.doi.org/10.1515/znb-2014-0208.

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AbstractThe title compound (5) was prepared by a reaction sequence starting from 2,3,4,5-tetramethoxytoluene (1) via the Blanc reaction, oxidation and alkylation. The described method provides a good yield of the C-6 heterocyclic-substituted benzoquinone derivative and is suitable for the synthesis of other benzoquinone derivatives.

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40

S, M. HASSAN, M. KHAFAGY M., A. EMAM H., and A. EL-MAGHRABY A. "Synthesis of New 2-Substituted-pyrazolo[4',3':5,6]pyrano[3,2-e][1,2,4]triazolo[ 1,5 -c ]pyrimidine Derivatives." Journal of Indian Chemical Society Vol. 74, Jan 1997 (1997): 27–29. https://doi.org/10.5281/zenodo.5876741.

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Chemistry Department. Faculty of Science. Al-Azhar University, Nasr City, Cairo, Egypt Manuscript received 3 November 1994, revised 3 April 1995 accepted 31 May 1995 1,3-Diphenylpyrazol-5-one has been reacted with arylidenemalononitriles (la d) to afford pyrano[2,3-cipyrazoles (2a-d). Reaction of 2d with triethyl orthoformate gives compound 4 which on hydrazinolysis yields aminoiminopyrhnidine derivative (5) Interaction of diffeient carboxylic acid derivatives with compound 5 gives 2-substituted-1,2,4-triazolopyrimidine derivatives (6-11).

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41

Musin, A. I., Yu G. Borisova, Sh Sh Dzhumaev, et al. "Synthesis and biological activity of 5-acetyl- and 5-hydroxyalkyl1,3-dioxane derivatives." Fine Chemical Technologies 18, no. 4 (2023): 381–91. http://dx.doi.org/10.32362/2410-6593-2023-18-4-381-391.

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Objectives. To synthesize derivatives of 5-acetyl- and 5-hydroxyalkyl-1,3-dioxanes and evaluate their effect on platelet aggregation and plasma hemostasis.Methods. To determine the qualitative and quantitative composition of the reaction masses, gas chromatography-, chromate mass spectrometry-, and 1H and 13C nuclear magnetic resonance spectrometry methods were used.Results. Derivatives of 5-acetyl- and 5-hydroxyalkyl-1,3-dioxanes were obtained under thermal heating conditions in order to evaluate their effect on platelet aggregation and plasma hemostasis.Conclusions. Derivatives of 5-acetyl- and 5-hydroxyalkyl-1,3-dioxanes were synthesized in high yields. Their effect on platelet aggregation and plasma hemostasis was established.

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42

Kurfürst, Antonín, Pavel Lhoták, Petr Nádeník, Františka Raclová-Pavlíková, and Josef Kuthan. "2-(Biphenyl-4-yl)-5-phenyl-1,3,4-oxadiazole (PBD): Electrophilic 4’-substitution and following transformations." Collection of Czechoslovak Chemical Communications 56, no. 7 (1991): 1495–504. http://dx.doi.org/10.1135/cccc19911495.

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PBD was converted into 4’-substituted derivatives I-XII using usual electrophilic reagents. The decomposition of PBD, 4’-acetyl derivative I and 4’-nitro derivative VI with hydroiodic acid gave 4’-substituted 4-biphenylcarboxylic acids XIIIa-XIIIc and benzoic acid, respectively. The regioselectivity of the reaction was also proved by means of high resolution NMR spectroscopy.

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43

Novak, Oksana, Tetiana Osadcha, and Oleksandr Petruk. "CONCEPT AND CLASSIFICATION OF DERIVATIVE FINANCIAL INSTRUMENTS AS A METHODOLOGICAL PRECISION ON THEIR REGULATION IN THE FINANCIAL SERVICES MARKET." Baltic Journal of Economic Studies 5, no. 3 (2019): 135. http://dx.doi.org/10.30525/2256-0742/2019-5-3-135-144.

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The urgency of the research topic is caused by the rapid growth of capital markets and the emergence of all new financial instruments, the complexity of their structure and the transition beyond the regulatory influence of supervisory authorities. Discussion issues on the identification of derivatives, as well as their certain types, create significant problems with their valuation, the correctness of accounting, and the application of regulatory measures. Inconsistency in the interpretation of derivative financial instruments nature and their certain types is also present in domestic legal acts. Therefore, until the elimination of these shortcomings, derivative financial instruments create additional risks for their owners – financial institutions, as well as for creditors and depositors. The purpose of the research, conducted in the article, lies in the clarification of derivatives nature and developing an appropriate classification of their types in order to its further use with a view of regulation. The methodological basis of the research. The methodological basis of the study is a dialectical approach to the understanding of the essence of derivative financial instruments; general scientific methods of knowledge of phenomena and processes (monographic, abstract-logical, synthesis, comparison, generalization), analysis of legal acts in the part of treatment of derivatives, derivative financial instruments and derivative securities, methods of grouping systematization and generalization in developing the classification of derivative financial instruments. Scientific results. It has been established that in order to maintain the stability of financial markets and their participants, the transformation of regulatory measures should be a permanent development and modification of the financial instruments that are being rotated. Various approaches to the interpretation of derivative financial instruments essence in normative legal acts and scientific literature have been analysed in order to improve the regulation of their issuance and circulation. This made it possible to streamline the conceptual apparatus and to group certain types of derivatives according to certain classification grounds. The basis for classification is the concept of “derivative financial instruments” as the broadest, which includes derivative securities and term contracts (derivatives). The concept of derivatives and derivative securities are delimited based on the study of terminology. It was established that derivatives are standard documents that certify the right and/or obligation to purchase or sell future securities, tangible or intangible assets, as well as funds or make payments on terms and conditions specified by them. However, in some cases, derivatives may acquire features of derivative securities, in particular, when issued through emission and freely traded in markets and bring income (losses) to their owner as a result of changes in their market value. The practical significance. The practical value of the research is the possibility of using the developed classification for the needs of emission regulation and the circulation of derivative financial instruments.

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M.A., METWALLY, Y. YOUSIF M., ISMAIEL A.M., and A. AMER F. "Syntheses of Some Arylsulphonyl Pyrazolines and Pyrazolones as Potential Antipyretic Analgesic Agents." Journal of Indian Chemical Society Vol. 62, Jan 1985 (1985): 54–56. https://doi.org/10.5281/zenodo.6302358.

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University of Mansoura, Mansoura, Egypt Manuscript received 21 February 1984, accepted 15 August 1984 Treatment of 3-methyl or 3-phenyl-2-pyrazolin-5-ones (1a, b) with p-acetamido or p-methylbenzenesulphonyl chloride afforded the O-sulphonyl derivatives (3a-d). The N-sulphonyl derivative (6) and N-methyl derivative (8) were also prepared. The 3- anilino derivatives (10a-d) and 3,5-dimethylpyrazoline derivative (13) were prepared. The ir spectral data of the synthesised compounds are discussed.

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45

Liu, Yin-Ping, and Zhi-Bin Li. "Homotopy Analysis Method for Nonlinear Differential Equations with Fractional Orders." Zeitschrift für Naturforschung A 63, no. 5-6 (2008): 241–47. http://dx.doi.org/10.1515/zna-2008-5-602.

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The aim of this paper is to solve nonlinear differential equations with fractional derivatives by the homotopy analysis method. The fractional derivative is described in Caputo’s sense. It shows that the homotopy analysis method not only is efficient for classical differential equations, but also is a powerful tool for dealing with nonlinear differential equations with fractional derivatives.

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46

Sultan Alwan, Ensaf, and Rafat Milad Mohareb. "Synthesis of bioactive heterocyclic compounds using camphor." Bulletin of the Chemical Society of Ethiopia 38, no. 4 (2024): 1069–76. http://dx.doi.org/10.4314/bcse.v38i4.20.

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The aim of the work was to synthesize novel heterocyclic compounds derived from camphor with antibacterial activity. The pyridazine, xanthene, pyranothiazole, pyridinothiazole, thiophene and pyrazole derivatives were produced from 4,11,11-trimethyl-9-phenyl-7-(2-phenylhydrazono)-3,4,5,6,7,9-hexahydro-1H-1,4-methanoxanthen-8(2H)-one (1). Thiophene derivatives 6a,b were produced according to the Gewald’s reaction for thiophene synthesis. On the other hand, pyranothiazol derivatives 8a,b were synthesized by the multicomponent reactions between xanthene derivative 5, benzaldehyde and ethylcyanoacetate or malononitrile in ethanol/triethylamine. Whereas, pyridinothiazole derivative 9 was produced in ethanol/ammonium acetate by the multicomponent reaction between xanthene derivative 5, benzaldehyde and malononitrile. The antibacterial activity of the synthesized compounds was evaluated against E. coli bacteria. All synthesized compounds showed moderate activity against E. coli bacteria. KEY WORDS: Anti-microbial, Camphor, Heterocyclic, Pyrazol-3(2H)-one, Thiazol-4(5H)-one, Thieno[3,2-d]thiazole, Xanthenes Bull. Chem. Soc. Ethiop. 2024, 38(4), 1069-1076. DOI: https://dx.doi.org/10.4314/bcse.v38i4.20

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47

Holý, Antonín, Ivan Rosenberg, and Hana Dvořáková. "Synthesis of (3-hydroxy-2-phosphonylmethoxypropyl) derivatives of heterocyclic bases." Collection of Czechoslovak Chemical Communications 54, no. 9 (1989): 2470–501. http://dx.doi.org/10.1135/cccc19892470.

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Analogs of the antiviral 9-(S)-(3-hydroxy-2-phosphonylmethoxypropyl)adenine (HPMPA, I), containing modified heterocyclic base, were prepared from racemic or (S)-N-(2,3-dihydroxypropyl) derivatives II. Compounds II are heated with chloromethylphosphonyl dichloride (XVII), the formed chloromethylphosphonylester chlorides of compounds II react with water to give a mixture of 2'- and 3'-chloromethylphosphonyl derivatives XVIII and XIX, respectively, which on isomerization by boiling with water in the arising acidic medium affords predominantly the 3'-isomer XIX. Treatment of this isomeric mixture with aqueous sodium hydroxide yields a mixture of 2'-O-phosphonylmethyl ethers (predominating, XXI) and 3'-O-phosphonylmethyl ethers of compounds II (XX). This approach has been applied to the synthesis of isomeric mixtures in the racemic as well as in the (S)-series derived from C-2, C-8 and N-6 substituted derivatives of adenine, from hypoxanthine and additional 6-substituted derivatives of purine, from guanine, 3-deazaadenine and other modified purine bases, from uracil, cytosine, their 5-methyl derivatives and 5-fluorouracil. Regioselective synthesis of compounds XXI was performed for biologically active derivatives (derivative of 2-aminoadenine (XXIe), guanine (XXIn), 3-deazaadenine (XXIp) and cytosine (XXIt)) as well as some other compounds (derivative of hypoxanthine (XXIj), uracil (XXIr), thymine (XXIs) and 5-methylcytosine (XXIu)): the former were obtained either from 3'-O-chloromethylphosphonyl derivatives XIX, isolated from the above-mentioned mixtures by ion-exchanger chromatography or HPLC, or by regioselective substitution, whereas the latter compounds were prepared by deamination (compound XXIj from adenine derivative I or the uracil and thymine derivatives XXIr and XXIu from the cytosine derivatives XXIt and XXIu). N-(S)-(3-Hydroxy-2-benzoyloxypropyl) derivative of N4-benzoylcytosine (XXIX) and N2-benzoylguanine (XXIV), obtained from compounds IIn and IIt by successive N-benzoylation, reaction with dimethoxytrityl chloride, benzoylation and mild acid treatment, were subjected to reaction with the chloride XVII and subsequent neutral and alkaline hydrolysis (compound XXIV), or to reaction with sodium methoxide followed by treatment with bromotrimethylsilane (compound XXIX), being thus converted into 1-(S)-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine (XXIt, HPMPC) and 9-(S)-(3-hydroxy-2-phosphonylmethoxypropyl)guanine (XXIn, HPMPG), respectively. The starting compounds (S)-II were synthesized from sodium salt of the corresponding heterocyclic base by reaction with 1-O-p-toluenesulfonyl-2,3-O-isopropylidene-(R)-glycerol (IIIa) (the (RS)-derivatives by reaction with 4-chloromethyl-2,2-dimethyl-1,3-dioxolane (IIIb)), followed by acid hydrolysis.

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48

Shao, Jiaan, Wenteng Chen, Di Ke, Ke Shu, En Chen, and Yongping Yu. "Highly Efficient Synthesis of Polysubstituted 2-Aminopyrroles via a Multicomponent Domino Reaction." Synlett 29, no. 07 (2018): 922–27. http://dx.doi.org/10.1055/s-0036-1591907.

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A highly efficient approach to polysubstituted 2-aminopyrroles containing a coumarin derivative unit at the 5-position of the pyrrole ring was developed via a novel multicomponent domino reaction of glyoxal monohydrate derivatives, anilines, coumarin derivatives, and malononitrile. This transformation proceeded via an α-aminoketone as the key intermediate.

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49

Spassova, Maria K., Antonín Holý, and Milena Masojídková. "Ribonucleosides of 3-amino- and 3,5-diaminopyrazole-4-carboxylic acid and their open-chain analogues: Synthesis and reactions." Collection of Czechoslovak Chemical Communications 51, no. 7 (1986): 1512–31. http://dx.doi.org/10.1135/cccc19861512.

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Bis(trimethylsilyl) derivative of ethyl 3-aminopyrazole-4-carboxylate (VI) and tris(trimethylsilyl) derivative of ethyl 3,5-diaminopyrazole-4-carboxylate (VII) on reaction with 2,3,5-tri-O-benzoyl-D-ribofuranolyl chloride and subsequent debenzoylation afforded the respective β-D-ribofuranosyl derivatives VIIIa and Xa. Their alkaline hydrolysis led to 1-(β-D-ribofuranosyl)-3-aminopyrazole-4-carboxylic acid (VIIIc) and 1-(β-D-ribofuranosyl)-3,5-diaminopyrazole-4-carboxylic acid (Xb). The esters VIIIa and Xa were not ammonolyzed under normal conditions. Contrary to nucleosidation of the silyl derivatives VI and VII, sodium salt of ethyl 3-aminopyrazole-4-carboxylate was alkylated with 4-chloromethyl-2,2-dimethyl-1,3-dioxolane (XI) or 5-(p-toluenesulfonyloxy)-1,3-dioxane (XVIIb) to give a mixture of the N-isomeric derivatives XIIIa, XIXa and XIIa, XVIIIa, respectively; sodium salt of the 3,5-diamino derivative V reacted with these synthons under formation of the corresponding compounds XIIIb and XXa. Subsequent alkaline and acid hydrolysis of XIIa and XIIIb gave the open-chain analogs of nucleosides XV and XVI. The N-(1,3-dioxan-5-yl) derivatives XVIIIc and XXa resisted acid hydrolysis, giving rise only to carboxylic acids XVIIIb and XXb.

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50

Sabzi, Noor Ali Hussein, and May Mohammed Jawad Al-Mudhafar. "Synthesis, characterization, and antimicrobial evaluation of new Schiff bases derived from vanillic acid conjugated to heterocyclic 4H-1,2,4-triazole-3-thiol." Pharmacia 70, no. 3 (2023): 657–63. http://dx.doi.org/10.3897/pharmacia.70.e104579.

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A multistep synthesis was established for the preparation of a new vanillic acid-1, 2, 4-1triazole-3-thiol conjugate (4). Finally, several aromatized aldehydes reacted with compound (4) to produce Schiff bases derivatives (5–11). The purpose of this research is to prepare new vanillic acid derivatives with 1, 2, 4-triazole-3-thiol heterocyclic ring structures and to evaluate their antimicrobial activity in a preliminary assessment. Fourier-transform infrared (FT-IR) and proton nuclear magnetic resonance spectroscopy (1H-NMR) were used to verify the structures of the newly synthesized compounds. all the final synthesized compounds (5–11) were tested for antimicrobial activity. The findings of this study demonstrate the viability of synthesizing vanillic acid combined with a 1, 2, 4-triazole-3-thiol ring derivative, which then reacted with various aldehydes to yield several new Schiff bases derivatives. Finally, the presence of an electron-withdrawing group at the fourth position (p- chloro group) of the aromatic ring improves the antibacterial activity of the derivative of the vanillic acid-triazole conjugate. Compound 8 with para chloro substituted Schiff base derivative showed potent activity when compared to other final derivatives but of no activity toward K. pneumonia.

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