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Journal articles on the topic '5-substituted-amino derivatives'

Author: Grafiati

Published: 4 June 2021

Last updated: 1 February 2022

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1

Yang, Minmin, and Stewart W. Schneller. "Amino substituted derivatives of 5′-amino-5′-deoxy-5′-noraristeromycin." Bioorganic & Medicinal Chemistry 13, no. 3 (February 2005): 877–82. http://dx.doi.org/10.1016/j.bmc.2004.10.031.

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2

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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3

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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4

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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5

El-Naggar, Mohamed, Abdel-Nasser El-Shorbagi, Dina H. Elnaggar, Abd El-Galil E. Amr, Mohamed A. Al-Omar, and Elsayed A. Elsayed. "Synthesis, Characterization, and Cytotoxic Evaluation of Some Newly Substituted Diazene Candidates." Journal of Chemistry 2018 (November 1, 2018): 1–9. http://dx.doi.org/10.1155/2018/3626824.

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A series of azocompounds containing methyl salicylate 4a–k and 1-naphthyl moiety 6–8 was synthesized and tested as anticancer agents. Nitrosation of methyl 5-amino-2-hydroxybenzoate or 1-aminonaphthalene by using NaNO2 in the presence of HCl afforded diazonium salt derivatives 2 and 5, which were treated with substituted imino or substituted amino derivatives, to give the corresponding substituted amino-pent-2-en-3-yl-diazenylbenzoate 4a–k or 2-substituted-1-(naphthalen-1-yl)diazene derivatives 6a–h, 7a,b, and 8a,b. All the synthesized compounds were elucidated by elemental analysis and spectroscopic evidence.

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6

Lahsasni, Siham, Dunya A. M. Al-Hemyari, Hazem A. Ghabbour, Yahia Nasser Mabkhoot, Fadilah S. Aleanizy, Asma A. Alothman, and Zainab M. Almarhoon. "Synthesis, Characterization, and Antibacterial and Anti-Inflammatory Activities of New Pyrimidine and Thiophene Derivatives." Journal of Chemistry 2018 (August 1, 2018): 1–11. http://dx.doi.org/10.1155/2018/8536063.

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Substituted[4,5]thieno[2,3-d]thiazolo[3,2-a]pyrimidin-5-one (3a–b) and pyrimidin-5(6H)-imine (3c–e) were synthesized via reaction of the starting compounds, ethyl 2-amino-substituted[b]thiophene-3-carboxylate (2a–c) and 2-amino-substituted [b]thiophene-3-carbonitrile (2d–f), respectively, with 2-bromothiazole. Synthesis of (bromo-substituted[b]thiophen-2-yl)alkanamide derivatives (4a–e) and thieno[2,3-d][1,3]oxazin-4-imine derivative (5) was accomplished via reaction of the starting compounds with bromoalkyl chloride through nucleophilic substitution; however, for the synthesis of compound 5, nucleophilic substitution was followed by nucleophilic addition to a nitrile group to form the oxazinimine ring. 1-(3-cyano-substituted[b]thiophen-2-yl)-3-(4-(trifluoromethyl)phenyl)thiourea derivatives (6a–c) were obtained via reaction of the starting compounds (2d–f) and 4-(trifluoromethyl phenyl)isothiocyanate. The lead compounds (2d–f) rapidly reacted with 4-(trifluoromethyl)benzaldehyde or 4-(2-pyridyl)benzaldehyde in acidic medium to yield compounds (7a–f) in large quantities. X-ray crystallography of compounds 4c and 7e confirmed their structures. Antimicrobial studies revealed that compound 6a was equally potent to ampicillin against Bacillus strains. Moreover, compounds 3e, 4d, and 6a possessed greater anti-inflammatory potency than that of the standard drug.

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7

Hussain, Sabir, Jyoti Sharma, and Mohd Amir. "Synthesis and Antimicrobial Activities of 1,2,4-Triazole and 1,3,4-Thiadiazole Derivatives of 5-Amino-2-Hydroxybenzoic Acid." E-Journal of Chemistry 5, no. 4 (2008): 963–68. http://dx.doi.org/10.1155/2008/924734.

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Various 4-amino-2-[4-(4-substituted phenyl)-5-sulfanyl-4H-1,2,4-triazol-3-yl] phenol (4a-c), 4-amino-2-{4-amino-5-[(4-substituted phenyl)amino]-4H-1,2,4-triazol-3-yl} phenol (5a-c) and 4-amino-2-{5-[(4-substituted phenyl)amino]-1,3,4-thiadiazole-2-yl} phenol (6a-g) were synthesized and evaluated for their antibacterial and antifungal activity. The compounds showed significant antibacterial activity againstS. aureus(gram-positive) andE.coli(gram-negative) bacteria and antifungal activity againstA. nigerfungi using cup plate technique

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8

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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9

Janeba, Zlatko, Antonín Holý, and Milena Masojídková. "Synthesis of Acyclic Nucleoside and Nucleotide Analogs Derived from 6-Amino-7H-purine-8(9H)-thione and 8-(Methylsulfanyl)adenine." Collection of Czechoslovak Chemical Communications 65, no. 11 (2000): 1698–712. http://dx.doi.org/10.1135/cccc20001698.

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Reaction of 8-bromoadenine derivatives 1 with thiourea in ethanol or butanol was used for the synthesis of the corresponding N9-substituted 6-amino-7H-purine-8(9H)-thiones 2. 8-(Methylsulfanyl)adenine derivatives 3 were prepared by reaction of thiones 2 with iodomethane in 1 M sodium methoxide or in aqueous 1.5 M potassium hydroxide. Alkylation of 6-amino-7H-purine-8(9H)-thione (2a) proceeds preferentially on the sulfur atom. Under similar conditions, alkylation of 8-(methylsulfanyl)adenine (3a) with diverse alkylation agents afforded N9-substituted adenine derivatives 3 and 6, and N3-substituted adenine derivatives 5 and 7. 8,3'-S-Anhydro derivatives 9 were prepared in good yields by cyclization of 6-amino-7H-purine-8(9H)-thiones 2d and 2f under the Mitsunobu reaction conditions.

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10

Prokopenko, V. M., S. G. Pil’o, and V. S. Brovarets. "Synthesis of 4-hetaryl-substituted 5-amino- and 5-sulfanyl-1,3-oxazole derivatives." Russian Journal of General Chemistry 81, no. 2 (February 2011): 405–10. http://dx.doi.org/10.1134/s1070363211020204.

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11

Mistry, K. M., and K. R. Desai. "Synthesis of Novel Heterocyclic 4-Thiazolidinone Derivatives and their Antibacterial Activity." E-Journal of Chemistry 1, no. 4 (2004): 189–93. http://dx.doi.org/10.1155/2004/590439.

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4-Thiazolidinones have been prepared by the reaction of various substituted Schiff bases 3 with Thioglycolic acid and Thiolactic acid. The intermediate Schiff bases 3 were synthesized by the condensation of various substituted 2-amino benzothiazole 1 with 1-(4'-methyl Phenyl)-3-methyl-5-pyrazolone 2. The starting compound substituted 2-amino benzothiazoles were prepared from various substituted amines via substituted phenyl thiourea. The structures of the compounds have been confirmed by elemental analysis and spectral analysis. The antibacterial activity of the compounds has also been screened againstStaphylococcus aureusandEscherichia coli.

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12

Dovlatyan, V. V., K. A. Eliazyan, V. A. Pivazyan, E. A. Kazaryan, and A. P. Engoyan. "Thiazolecarboxylic Acid Derivatives. 1. N-Substituted 2-Amino-4-methylthiazole-5-carboxylic Acid Derivatives." Chemistry of Heterocyclic Compounds 40, no. 1 (January 2004): 84–89. http://dx.doi.org/10.1023/b:cohc.0000023773.23834.ba.

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13

Neelgundmath, Mahabaleshwaraiah, and Oblennavar Kotresh. "Synthesis, Evaluation and Characterization of Some 1,3,4-Triazole-2-one Derivatives as Antimicrobial Agents." E-Journal of Chemistry 9, no. 4 (2012): 2407–14. http://dx.doi.org/10.1155/2012/672125.

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A series of novel compounds like 3[(phenyl substituted)-5-methyl-1(Benzosulphonylamine)]-1,3,4-triazole-2-ones II(a-f) were synthesized by treating 4-amino-1-phenyl-3-methyl-5-oxo-1,2,4-triazoles with benzene sulphonyl chloride using pyridine as solvent. Similarly by using 4-amino-1-aryl-3-methyl-5-oxo-1,2,4-triazoles and acetic anhydride as starting material 3[(phenyl substituted)-5-methyl-1(acetylamino)]-1,3,4-triazole-2-ones III(a-f) were synthesized and also 3[(phenyl substituted)-5-methyl-1(chloroacetyl)]-1,3,4-triazole-2-ones I(a-f) were synthesized by treating 4-amino-1-aryl-3-methyl-5-oxo-1,2,4-triazoles with chloroacetyl chloride in presence of a non-polar solvent like benzene. Elemental analysis, GCMS, IR, and1H NMR confirmed the structures of the newly synthesised compounds. The newly synthesized compounds are also screened for their antibacterial, antifungal and anti-inflammatory activities.

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14

Mariah, Fatma El. "Synthesis, Reactions and Antimicrobial Activity of Thieno[2,3-c]pyridazine Derivatives." Journal of Chemical Research 2009, no. 10 (October 2009): 593–98. http://dx.doi.org/10.3184/030823409x12508790019612.

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The reaction of N1-(un)substituted 4-aminosulfonamide with 6-chloropyridothienopyridazine (5) and 8-chloro-pyrimidothienopyridazine (14) gave 6-substituted aminopyridothienopyridazine (9) and 8-substituted amino-pyrimidothienopyridazine (16) respectively. All of the derivatives have been characterised by analytical and spectroscopic studies and also tested for their in vitro antibacterial and antifungal activity against a variety of microorganisms.

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15

Neumann, Helfried, Stefan Klaus, Markus Klawonn, Dirk Strübing, Sandra Hübner, Dirk Gördes, Axel Jacobi von Wangelin, Michael Lalk, and Matthias Beller. "A New Efficient Synthesis of Substituted Luminols Using Multicomponent Reactions." Zeitschrift für Naturforschung B 59, no. 4 (April 1, 2004): 431–38. http://dx.doi.org/10.1515/znb-2004-0411.

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AbstractA new general synthesis of substituted luminols (5-amino-2,3-dihydrophthalazine-1,4-diones) is presented. Diversely substituted luminol derivatives can be synthesized in three steps. The products are of interest as new materials, which exhibit chemiluminescence.

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16

Shilin, S., Z. Voitenko, and M. Nechai. "SYNTHETIC PYRIDINE SUBSTITUTED AMINO ACIDS AND THEIR DERIVATIVES." Bulletin of Taras Shevchenko National University of Kyiv. Chemistry, no. 1(56) (2019): 22–25. http://dx.doi.org/10.17721/1728-2209.2019.1(56).5.

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This paper reports on the synthesis of new derivatives of ε-aminocaproic and γ-aminobutyric acid modified with a pyridin-2-yl substituent at the ω-position of the main chain. The hemostatic activity of both ε-aminocaproic acid itself and its various synthetic analogues is widely known. Likewise, numerous γ-aminobutyric acid derivatives are strong neurotransmitters extensively used in the treatment of the nervous system disorders. No less popular are biologically active substances containing a pyridine or piperidine fragment; among which there are antibiotics, antimalarial, anti-sclerotic and antiallergic drugs, as well as anti-depressants and analgesics. Therefore, the introduction of the pyridine fragment into the amino acid structures is interesting in terms of their potential biological activity investigation. So, a method for the synthesis of 5-amino-5-(pyridin-2-yl)pentanoic and 6-amino-6-(pyridin-2-yl)hexanoic acid has been developed by us. The proposed scheme is based on the available reagents using. The key stage is the Schmidt rearrangement of 2-(pyridin-2-yl)cyclopentanone and 2-(pyridin-2-yl)cyclohexanone, previously synthesized from pyridine N-oxide and cycloalkenyl morpholinide. For synthesized pyridine substituted cycloalkanones according to NMR spectroscopy, the presence of keto-enol tautomerism was established. As a result of Schmidt rearrangement, lactams (2-(pyridin-2-yl)piperidone and 2-(pyridin-2-yl)azepanone) are formed, and the last ones had been hydrolyzed in an acidic medium to open the lactam cycle. Thus, 5-amino-5-(pyridin-2-yl)pentanoic and 6-amino-6-(pyridin-2-yl)hexanoic acid were isolated as hydrochlorides and the hydrochlorides were converted to the zwitterion form using propylene oxide. The first stage of the developed scheme (preparation of pyridylalkanones) occurs in rather low yields, about 35 %. But, after the rearrangement, hydrolysis and the formation of zwitterion do not cause difficulties and are characterized by high yields. Consequently, the proposed synthetic sequence is preparatively advantageous.

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17

Galkina, I. V., G. L. Takhautdinova, K. A. Ivshin, Kh R. Khayarov, D. R. Islamov, Yu V. Bakhtiyarova, L. N. Yamalieva, O. N. Kataeva, and V. I. Galkin. "5-Amino-Substituted Derivatives of 4-Nitrofurazane: Synthesis, Structure, and Biological Activity." Russian Journal of General Chemistry 88, no. 5 (May 2018): 898–902. http://dx.doi.org/10.1134/s1070363218050092.

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18

Ispikoudi, Maria, Michalis Amvrazis, Christos Kontogiorgis, Alexandros E. Koumbis, Konstantinos E. Litinas, Dimitra Hadjipavlou-Litina, and Konstantina C. Fylaktakidou. "Convenient synthesis and biological profile of 5-amino-substituted 1,2,4-oxadiazole derivatives." European Journal of Medicinal Chemistry 45, no. 12 (December 2010): 5635–45. http://dx.doi.org/10.1016/j.ejmech.2010.09.016.

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19

Slavinskaya, V. A., D. �. Sile, M. Yu Katkevich, �. Kh Korchagova, and �. Lukevits. "Synthesis of?-substituted?-amino acids by the alkylation of 5-oxazolinone derivatives." Chemistry of Heterocyclic Compounds 30, no. 6 (June 1994): 724–28. http://dx.doi.org/10.1007/bf01166316.

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20

Ghorab, Mostafa M., Zienab H. Ismail, Awwad A. Radwan, and Mohamad Abdalla. "Synthesis and pharmacophore modeling of novel quinazolines bearing a biologically active sulfonamide moiety." Acta Pharmaceutica 63, no. 1 (March 1, 2013): 1–18. http://dx.doi.org/10.2478/acph-2013-0006.

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In the present work, interaction of the strategic starting material, methyl 2-isothiocyanatobenzoate (1), with sulfa drugs resulted in the formation of methyl 2-[3-(4-(N-substituted sulfamoyl)phenyl)thioureido] benzoates 2-5, which upon reaction with hydrazine hydrate afforded N-amino derivatives 6-9. Triazoloquinazoline derivatives 10-18 were obtained via reaction of compounds 6-8 with aromatic aldehydes. Also, the reaction of compound 8 with formic acid gave the corresponding triazoloquinazoline derivative 19. Triazinoquinazoline derivatives 22, 23 were obtained via reaction of N-amino derivatives 6 or 8 with ethyl chloroacetate. Interaction of 6 with diethyloxalate yielded triazoloquinazoline 26. The synthesized compounds were screened for their in vitro antimicrobial activities and some of them exhibited promising antibacterial activity compared to ampicillin as positive control. Compounds that revealed significant activity are able to satisfy effectively the proposed pharmacophore geometry.

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21

Youssef, Ahmed Said Ahmed. "Reactions of 2-amino-4,5,6,7-tetrahydro[1]benzothiophene-3-carbonitrile and 6-amino-1,4-dihydro-3-methyl-1,4-diphenylpyrano[2,3-c]pyrazole-5-carbonitrile with substituted benzylidenemalononitriles, α,β-acetylenic esters and ketones." Journal of Chemical Research 2009, no. 4 (April 2009): 214–17. http://dx.doi.org/10.3184/030823409x435874.

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Reactions of 2-amino-4,5,6,7-tetrahydro[1]benzothiophene-3-carbonitrile (1a) with substituted benzylidenemalononitriles gave 4-amino-2-(1-cyano-2-arylvinyl)benzothieno[2,3- d]pyrimidine derivatives (3) as ( E,Z)-mixtures and in one case (2c) as separated ( Z)- and ( E)-isomers. Similar treatment of 6-amino-1,4-dihydro-3-methyl-1,4-diphenyl-pyrano[2,3- c]pyrazole-5-carbonitrile (4) yielded similarly-formed pyrazolopyranopyrimidine derivatives (5a, b) as ( Z)-and ( E)-stereoisomers. Attempted acetylation of the aminobenzothienopyrimidines resulted in degradation of the pyrimidine ring and the formation of N-(3-cyano-4,5,6,7-tetrahydro[1]benzothien-2-yl)acetamide (1b). Treatment of 4 with acetylenic esters and ketones (6a-d) afforded the ( Z)-substituted enaminopyrano[2,3- c]pyrazole derivatives. Reacting 1a with aroyl phenyl acetylenes gave by Michael addition the enamino-ketones (8a-c).

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22

Swarnkar, Pawan Kumar, P. Kriplani, G. N. Gupta, and K. G. Ojha. "Synthesis and Antibacterial Activity of Some New Phenothiazine Derivatives." E-Journal of Chemistry 4, no. 1 (2007): 14–20. http://dx.doi.org/10.1155/2007/402673.

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A series of some new phenothiazine derivatives were synthesized with the objective for evaluation as antimicrobials. The title compounds were prepared by a five step synthesis scheme. 2-Amino-6-substituted benzothiazoles (1) on diazotization afford 6-substituted benzothiazolyl-2-diazonium chlorides (2). Reaction of 2 with cold solution ofβ-naphthol in dilute NaOH furnishesα-(2-diazo-6-substituted benzothiazolyl)-β-sodionaphthoxides (3) which on acidification with concentrated HCl givesα-(2-diazo-6-substituted benzothiazolyl)-β-naphthols (4). Reaction of 4 with p-substituted anilines givesα-(2-diazo-6-substituted benzothiazolyl)-β-(p-substituted anilino) naphthalenes (5). This synthesis besides by using conventional methods was also attempted using microwave. Fusion of 5 with sulphur in presence of iodine results inα-(2-diazo-6-substituted benzothiazolyl)-6- substituted [2, 3-b] benzophenothiazines(6). The structures of all these compounds have been supported by elemental analysis and their spectral studies. All synthesized compounds were tested for their antibacterial activity using standard drugs.

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23

Yu, Hong Mei, Hai Feng Li, Hong Min Jia, and Xiu Hui Zhu. "Synthesis of 2-Chloro-4,6-Diamino-5-Cyanopyrimidine and its Amino-Substituted Derivatives." Advanced Materials Research 233-235 (May 2011): 321–24. http://dx.doi.org/10.4028/www.scientific.net/amr.233-235.321.

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The important pyrimidine intermediate 2-chloro-4,6-diamino-5-cyanopyrimidine was prepared by the cyclization of sodium salt of 1-amino-1-cyanamino-2,2-dicyanoethylene which was obtained from sodium dicyanamide and malononitrile via the nucleophilic addition in good yield and purity. The 4,6-diamino-5-cyanopyrimidines substituted with different amino groups could be synthesized by nucleophilic substitution reaction of amines, and they have good bactericidal activities to some funguses.

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24

Jílek, Jiří, Jiří Urban, Vojtěch Kmoníček, Josef Pomykáček, Jiří Holubek, Emil Svátek, Oluše Matoušová, et al. "Potential anticonvulsants: 3-Chlorobenzophenone derivatives." Collection of Czechoslovak Chemical Communications 54, no. 8 (1989): 2248–60. http://dx.doi.org/10.1135/cccc19892248.

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Reactions of 2-(2-iodoacetamido)-5-chlorobenzophenone with 2-amino-2-phenylethanol, 2-amino-1-phenylethanol, 3-amino-2-phenylpropanol, D-(+)-norpseudoephedrine, and 2-aminopropane-2-carbonitrile gave the 2-substituted N-(2-benzoyl-4-chlorophenyl)acetamides X-XIV. 2,3'-Dichlorobenzhydrol (XVI) and 2,3'-dichlorobenzhydryl chloride (XIX) were transformed to the ethers XVII and XVIII and to the amines XXI-XXIV. Compound XVI was oxidized to the ketone XXV which was transformed via the oxime XXVI to compound XXVII. The basic products were converted to salts which were pharmacologically tested. Compounds X, XVII, XXIII, and XXVII showed anticonvulsant effects and some other neurotropic activities.

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25

Huppatz, JL. "Systemic Fungicides. The Synthesis of Pyrazolo[1,5-a]pyrimidine Analogues of Carboxin." Australian Journal of Chemistry 38, no. 1 (1985): 221. http://dx.doi.org/10.1071/ch9850221.

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The synthesis of a series of pyrazolo [1,5-a] pyrimidine derivatives, structural analogues of the systemic fungicide carboxin, is described. A common intermediate incorporating structural features desirable for fungicidal activity, N-phenyl-3(5)-amino-5(3)-methylpyrazole-4- carboxamide (6), was used to prepare pyrazolo [1,5-a] pyrimidines variously substituted in positions 5 and 7 of the ring system. Bromination of N-phenyl-2-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide (8) occurred preferentially in the phenyl ring and the 6-bromo derivative was prepared by bromination of the corresponding 3-ethoxycarbonyl derivative (24). Attempted nitration of the ester (24) resulted in displacement of the ethoxycarbonyl substituent by a nitro group. The simplest pyrazolo [1,5-a] pyrimidine (8) showed a high level of fungicidal acitvity in fungal growth assays of Basidiomycete species, but compounds substituted in the pyrimidine ring were inactive.

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26

Kosaraju Lahari and Raja Sundararajan. "Design, Synthesis, Characterisation & Anticonvulsant Activities of Novel Heterocyclic Substituted Isatin Derivatives." International Journal of Research in Pharmaceutical Sciences 11, no. 4 (October 13, 2020): 6351–62. http://dx.doi.org/10.26452/ijrps.v11i4.3392.

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Twelve new isoxazole/pyrazole/pyrimidine substituted 5-nitrosation analogues were designed according to the requirements of the anticonvulsant drugs pharmacophore model and synthesised from indole-2,3-dione. Entire prepared compounds chemical structures were established from its IR, proton-NMR, Mass spectrum & microanalysis data. Anticonvulsant potency of final isatin analogues was assessed by MES technique & sc PTZ technique. Besides rotarod test was used to assess the neurotoxicity of all potent title analogues. Title compounds exhibited a varying degree of anticonvulsant potency ranging from mild to good. In the present study, it was concluded that pyrazole derivatives exhibited higher anti-epileptic activity than isoxazole derivatives. However, pyrimidine analogues displayed inferior activity than isoxazole analogues. 4-(2-(4-(1-((Dimethylamino)methyl)-5-nitro-2-oxindole-3-ylideneamino)phenyl) hydrazone)-1-(4-chlorophenyl)-3-amino-1H-pyrazole-5(4H)-one 7c was established as the most active analog of this series. Hence this derivative can act as a pilot molecule for further progress of new effective anticonvulsant drugs.

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27

Rajeswar Rao, V., M. S. Rao, and T. V. Padmanabha Rao. "A novel synthesis of thiazolyl, imidazothiadiazolyl, and thiadiazinyl-2H-1-benzopyran-2-ones." Collection of Czechoslovak Chemical Communications 51, no. 10 (1986): 2214–21. http://dx.doi.org/10.1135/cccc19862214.

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3-Acetylcoumarins I with arylthiourea in the presence of iodine gave substituted 3-(2-arylamino-4-thiazolyl)-2H-1-benzopyran-2-ones (IIa-IIc). The structures of these products have been confirmed and they were converted into acetyl derivatives (IId-IIf). Condensation of various 3-(2-bromoacetyl)-2H-1-benzopyran-2-ones (III) with 2-amino-6-substituted thiadiazoles IV in the presence of ethanol and dimethylformamide yielded substituted 3-(2-substituted imidazo[2,1-b]thiadiazol-6-yl)-2H-1-benzopyran-2-ones (VI). Reaction of III with 3-substituted 4-amino-5-mercapto-S-triazole VII resulted in the formation of VIII in a single step.

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28

Mahdi, Monther. "Synthesis, Characterization and Antimicrobial Activity of Some Novel 1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile Derivatives." JOURNAL OF ADVANCES IN CHEMISTRY 11, no. 6 (September 16, 2015): 3635–41. http://dx.doi.org/10.24297/jac.v11i6.851.

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The present research work deals with synthesize a series of various substituted benzothiazole containing 6-amino- 4-(substituted aryl)- tetrahydropyrano[2,3-c]pyrazole-5-carbonitrilic by reacting 2-mercaptobenzothiazole with hydrazine hydrate to synthesize hydrazine derivatives of benzothiazole (1), which then reacted with β- keto ester to develop pyrazole derivative (2), and then finally reacted with malononitrile and different aromatic aldehydes to obtain the final compounds (3a-3f). The structures of the intermediates and final compounds are assigned by using FTIR and 1H-NMR. The final compounds were screened for their antibacterial activity against four tested bacteria as G+ and G- using a well diffusion method. The results of antibacterial activity exhibited that the species Klebsiella pneumonia was the most effected types, while Pseudomonas aeruginosa was least the effected in general.

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29

Hwang, Kijun, Namkyu Choi, and Inho Cho. "ChemInform Abstract: Nonprotein Amino Acids: Preparation of 5-Substituted-2-aminoadipic Acid Derivatives." ChemInform 30, no. 28 (June 14, 2010): no. http://dx.doi.org/10.1002/chin.199928099.

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30

Rutjes, Floris P., Bart C. van Esseveldt, Floris L. van Delft, Jan M. Smits, and René de Gelder. "Pd-Catalysed Synthesis of 5-Substituted Proline Derivatives from Acetylene-Containing Amino Acids." Synlett, no. 15 (2003): 2354–58. http://dx.doi.org/10.1055/s-2003-43337.

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31

Voitekhovich, S. V., A. N. Vorob'ev, P. N. Gaponik, and O. A. Ivashkevich. "Synthesis of New Functionally Substituted 1-R-tetrazoles and Their 5-Amino Derivatives." Chemistry of Heterocyclic Compounds 41, no. 8 (August 2005): 999–1004. http://dx.doi.org/10.1007/s10593-005-0267-4.

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32

Thomas, Joice, Alenka Jejcic, Peter Vervaeke, Romeo Romagnoli, Sandra Liekens, Jan Balzarini, and Wim Dehaen. "Structure-Activity Relationship of Tumor-Selective 5-Substituted 2-Amino-3-carboxymethylthiophene Derivatives." ChemMedChem 9, no. 12 (September 18, 2014): 2744–53. http://dx.doi.org/10.1002/cmdc.201402274.

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33

Wang, Ming-Shu, Yi Gong, Zhi-Cheng Yu, Yan-Guang Tian, Lin-Sheng Zhuo, Wei Huang, and Neng-Fang She. "Grignard Reagent Utilization Enables a Practical and Scalable Construction of 3-Substituted 5-Chloro-1,6-naphthyridin-4-one Derivatives." Molecules 25, no. 23 (December 1, 2020): 5667. http://dx.doi.org/10.3390/molecules25235667.

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A robust, practical, and scalable approach for the construction of 3-substituted 5-chloro-1,6-naphthyridin-4-one derivatives 13 via the addition of Grignard reagents to 4-amino-2-chloronicotinonitrile (15) was developed. Starting with various Grignard reagents, a wide range of 3-substituted 5-chloro-1,6-naphthyridin-4-one derivatives 13 were conveniently synthesized in moderate-to-good yields through addition–acidolysis–cyclocondensation. In addition, the robustness and applicability of this synthetic route was proven on a 100 g scale, which would enable convenient sample preparation in the preclinical development of 1,6-naphthyridin-4-one-based MET-targeting antitumor drug candidates.

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34

Mohana, Kikkeri N., and Chikkur B. Pradeep Kumar. "Synthesis and Antioxidant Activity of 2-Amino-5-methylthiazol Derivatives Containing 1,3,4-Oxadiazole-2-thiol Moiety." ISRN Organic Chemistry 2013 (August 19, 2013): 1–8. http://dx.doi.org/10.1155/2013/620718.

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A series of new 5-(2-amino-5-methylthiazol-4-yl)-1,3,4-oxadiazole-2-thiol derivatives 6(a–j) were designed and synthesized with various substituted aldehydes. The chemical structures were confirmed by elemental analyses, FT-IR, 1H NMR, and mass spectral studies. The antioxidant activity of the synthesized compounds was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl, nitric oxide, and superoxide radical scavenging assay methods. Compounds 6a, 6e, and 6c showed significant radical scavenging potential due to the presence of electron donating substituent on substituted aldehydes.

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35

Liu, Huang, Chen, Li, Yan, Jin, and Xu. "Ionic Liquids Enhanced Alkynyl Schiff Bases Derivatives of Fipronil Synthesis and Their Cytotoxicity Studies." Molecules 24, no. 18 (September 4, 2019): 3223. http://dx.doi.org/10.3390/molecules24183223.

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To obtain highly selective toxic derivatives of fipronil, a series of Schiff bases with an alkynyl group (3a–3k) were designed and synthesized from 4-ethynylbenzaldehyde (2) and 4-substituted 5-amino-N-arylpyrazole (1a–1k) via a nucleophilic addition elimination reaction in ionic liquids. Utilization of ionic liquids was demonstrated to endow the yield of each compound beyond 50%, which was enhanced over 1.5 times of the synthetic productive rates comparing the conventional method by which longer reactive time was consumed. The derivatives were characterized via nuclear magnetic resonance hydrogen spectroscopy (1H-NMR), carbon-13 nuclear magnetic resonance spectroscopy (13C-NMR), and electrospray ionization high resolution mass spectrometry (ESI-HRMS). The cytotoxicity of these derivatives on Trichoplusia ni (Hi-5) cell and Spodoptera litura cell (SL cell) was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) bioassays. The results indicated that several compounds had potential cytotoxicity on Hi-5 cell, especially a 4-ethyl substituted alkynyl Schiff base derivative (3f) that was demonstrated to possess high selective toxicity to the Hi-5 cell than the SL cell. In addition, 3f exhibited comparable toxic activity to commercial fipronil on a Hi-5 cell while a little toxic effect on the SL cell, which satisfied the expectation for selective toxicity screening.

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36

Riyadh, Sayed M., and Sobhi M. Gomha. "Two decades of the synthesis of mono- and bis-aminomercapto[1,2,4]triazoles." RSC Advances 10, no. 42 (2020): 24994–5012. http://dx.doi.org/10.1039/d0ra04208k.

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4-Amino-5-mercapto[1,2,4]triazole and its 3-substituted derivatives have proven to be of biological interest and provide access to a new class of biologically active heterocyclic compounds for biomedical applications.

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37

Hanna, Naeem B., Milena Masojídková, Pavel Fiedler, and Alois Pískala. "Synthesis of Some 6-Substituted 5-Azacytidines." Collection of Czechoslovak Chemical Communications 63, no. 2 (1998): 222–30. http://dx.doi.org/10.1135/cccc19980222.

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Protected 6-substituted benzyl, phenyl and chloromethyl derivatives of 5-azacytidine 8-10 have been prepared by addition of phenylacetyl- (2), benzoyl- (3) or (chloroacetyl)guanidine (4) to 2,3,5-tri-O-benzoyl-β-D-ribosyl isocyanate (1) and subsequent silylation-mediated cyclization of the obtained acyl(carbamoyl)guanidines 5-7. 4-Amino-6-phenyl-1,3,5-triazin-2(1H)-one (12) was obtained by condensation of carbamoylguanidine (13) with methyl benzoate in presence of methanolic sodium methoxide or by condensation of 13 with triethyl orthobenzoate in N,N-dimethylformamide. Stannic chloride catalyzed condensation of silylated 6-phenyl derivative 11 with 1-O-acetyl-2,3,5-tri-O-benzoyl-β-D-ribose (14) in 1,2-dichloroethane afforded a 1.2 : 1 mixture of N1 and N3 nucleosides 9 and 15, respectively. Methanolysis of the protected compounds 8-10 and 15 gave the respective free nucleosides 16-19. The latter compounds inhibited the growth of bacteria E. coli B to a much lower extent than the unsubstituted 5-azacytidine.

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38

Nurkenov, O. A., S. D. Fazylov, T. M. Seilkhanov, Zh Nurmaganbetov, A. M. Gazaliev, and G. Zh Karipova. "Synthesis and structure of thiourea derivatives of functionally substituted pyridines." Bulletin of the Karaganda University. "Chemistry" series 101, no. 1 (March 30, 2021): 4–11. http://dx.doi.org/10.31489/2021ch1/4-11.

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The article presents data on the synthesis and study of the structure of thiourea derivatives of functionally substituted pyridines. New thiourea derivatives containing a pharmacologically active pyridine moiety in their structure were obtained. As the starting synton, 2-amino-5-bromopyridine, 2-amino-3-hydroxypyridine and 2-aminomethylpyridine were selected. It was shown that the interaction of 2-amino-5-bromopyridine, 2-amino-3-hydroxypyridine and 2-aminomethylpyridine with ethyl and phenylisothiocyanates in ethanol leads to the formation of the corresponding pyridine-containing thioureas. The synthesis of the initial isothiocyanates was carriedout in situ from the corresponding acidic chlorides (benzoyl chloride and p-brombenzoyl chloride) by heating them with potassium thiocyanate in acetone. The structure of the synthe-sized compounds was studied by 1H and 13C NMR spectroscopy, as well as by the data of two-dimensional spectra of COSY (1H-1H) and HMQC (1H-13C). The values of chemical shifts, multiplicity, and integrated in-tensity of 1H and 13C signals in one-dimensional NMR spectra were determined. Using spectra in the formats COSY (1Н-1Н) and HMQC (1Н-13С), homo-and heteronuclear interactions were established, confirming the structure of the studied compounds.

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39

Kumar, Jat Rakesh, Jat Jawahar L., and D. P. Pathak. "Synthesis of Benzimidazole Derivatives: As Anti-hypertensive Agents." E-Journal of Chemistry 3, no. 4 (2006): 278–85. http://dx.doi.org/10.1155/2006/765712.

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A new series of non peptide angiotensin(A-II) receptor antagonist has been prepared. ThisN-(biphenyl methyl) imidazolese.g. 5-substituted (amino) -2- phenyl-1-(2ʼcarboxy biphenyl-4-yl) benzimidazoles differ from the previously reported and related compounds in that they produce a potent hypertensive effect upon oral administration. The earlier series were generally active only when administered intravenously. It has been found that 2’-position of biphenyl is essential. Only ortho substituted acid possess both high affinity for the AII receptor and oral anti-hypertensive potency.

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40

Ahmad, Roshan, Rukhsana Jabeen, Mohammad Zia-ul-Haq, Humaira Nadeem, Helmut Duddeck, and Eugen J. Verspohl. "Chiral Aryl Sulfonyl Hydantoins as Hypoglycemic Agents." Zeitschrift für Naturforschung B 55, no. 2 (February 1, 2000): 203–7. http://dx.doi.org/10.1515/znb-2000-0212.

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Some novel chiral sulfonyl hydantoin derivatives 2a-e and 3 a-e have been prepared. p-Toluenesulfonyl chloride on treatment with L-amino acids in presence of K2CO3/H2O yielded N-(p-toluensulfonyl-)amino acids 1a - e which were cyclized in presence of NH4-SCN Ac2O to afford 1-(p-toluenesulfonyl)-5-substituted-2-thiohydantoins 2a-e. These compounds were oxidized with HNO3 to yield 1-(p-toluenesulfonyl)-5-substituted hydantoins 3a-e. The enantiomeric ratios of 3a-e were determined by 1H NMR spectroscopy using Eu(hfc)3. The antidiabetic activity of 3a-d has been determined.

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41

Liu, Ju, Xue-Chen Hao, Ye Chen, Shi Ding, Hong-Sheng Liu, and Dan Wang. "Synthesis of New Substituted 5-amino-8H-phthalazino[1,2-b]quinazolin-8-one Derivatives." Journal of Chemical Research 41, no. 1 (January 2017): 18–20. http://dx.doi.org/10.3184/174751917x14815427219167.

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A series of novel substituted 5-amino-8 H-phthalazino[1,2- b]quinazolin-8-one derivatives synthesised by condensation of different amines with 5-chloro-8 H-phthalazino[1,2- b]quinazolin-8-one, which was prepared from methyl 2-aminobenzoate by condensation with hydrazine hydrate and then cyclisation with a phthalic anhydride in N,N-dimethylacetamide at refluxing condition. The intermediate and target compounds were obtained in good yields and were easily purified by filtration or recrystallisation.

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42

Hassan, Alaa A., Yusria R. Ibrahim, and Ahmed M. Shawky. "Reactions of Substituted Carbohydrazides with Electron-poor Olefins." Zeitschrift für Naturforschung B 63, no. 8 (August 1, 2008): 998–1004. http://dx.doi.org/10.1515/znb-2008-0813.

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Substituted carbohydrazides 1a - e reacted with ethenetetracarbonitrile (2) in dimethylformamide with formation of diacylhydrazines 4a - e and 5-amino-1-substiuted pyrazole-3,3,4-tricarbonitriles 5a - e. On the other hand, 1a-c reacted with diethyl (E)-2,3-dicyanobutenedioate (3) to give oxadiazinone and pyrazolone derivatives 12a - e and 13a - e, respectively.

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43

Habibi, Azizollah, Sahar Khosravi, Seyyed M. Shahcheragh, and Mohd B. Abdul Rahman. "One-Pot Green Synthesis of Some Novel N-Substituted 5-Amino-1,3,4- Thiadiazole Derivatives." Letters in Organic Chemistry 17, no. 7 (July 7, 2020): 517–22. http://dx.doi.org/10.2174/1570178616666190926105533.

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In the current study, a green, one-pot, three-component reaction was performed to prepare novel N-substituted 5-amino-1,3,4-thiadiazole derivatives. The thiadiazoles were obtained from the reaction of a ketene S,S-acetal of Meldrum’s acid or barbituric acid (as key intermediates), hydrazine, and isothiocyanate. The key advantages of this manner include environmentally safe reactions, high yield, appropriate reaction time, simple reaction conditions, and use of a green reaction solvent. The structure of thiadiazoles was determined based on the spectroscopic data.

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44

Abdel-Latif, Fathy F., Kamal M. El-Shaieb, and Ahmed G. El-Deen. "An Efficient and Simple Route to Prospective Biologically Active Isoindoloquinazoline, Pyrimidine and Thiazine Derivatives Using 2-Amino-N-Arylbenzamidine and Related Compounds as Starting Materials." Zeitschrift für Naturforschung B 66, no. 9 (September 1, 2011): 965–71. http://dx.doi.org/10.1515/znb-2011-0916.

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The reaction of (Z)-2-amino-N`-arylbenzamidines 1, 2-amino-4,5,6,7-tetrahydrobenzo[b]-thiophene-3-carboxamide (4) and 4-amino-5-substituted-2-(phenylamino)thiophene-3-carboxamides 12 with o-phthalaldehyde (2), terephthalaldehyde (9), and 4-formyl[2.2]paracyclophane (16) in ethanol under reflux conditions afforded isoindoloquinazoline, thienopyrimidine, pyrimidine and thiazine derivatives, respectively. The products were characterized based on their spectroscopic data and elemental analysis.

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45

Ahmed, Hatem Abdel Moniem. "A Facile One-pot Synthesis of New Pyrazolopyrimidines and Pyrazolo Pyridines Derivatives." JOURNAL OF ADVANCES IN CHEMISTRY 8, no. 1 (March 12, 2014): 1533–38. http://dx.doi.org/10.24297/jac.v8i1.6789.

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A Simple Facile One-pot reaction, novel and efficient rout for the synthesis of substituted pyrazolo [3, 4-d] pyrimidines, and pyrazolo [3, 4-b] pyridines, results from reaction of substituted-5-amino-4-cyanopyrazoles with malononitrile and diethylmalonate respectively. The structures of the products and conceivable mechanisms are discussed. The antibacterial activity of some new synthesized compounds was evaluated and seemed to be significant.

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46

Quesada, Antonio, Antonio Marchal, Manuel Melguizo, Manuel Nogueras, Adolfo Sánchez, John N. Low, Debbie Cannon, Dorcas M. M. Farrell, and Christopher Glidewell. "Amino-substituted O6-benzyl-5-nitrosopyrimidines: interplay of molecular, molecular-electronic and supramolecular structures." Acta Crystallographica Section B Structural Science 58, no. 2 (March 25, 2002): 300–315. http://dx.doi.org/10.1107/s0108768101021607.

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The structures of eight 2,4,6-trisubstituted-5-nitrosopyrimidines (one of which crystallizes in two polymorphs) have been determined, including seven O6-benzyl derivatives which are potential, or proven, in vitro inhibitors of the human DNA-repair protein O6-alkylguanine-DNA-transferase. In the derivatives having an amino substituent at the 4-position, an intramolecular N—H...O hydrogen bond with the nitroso O as an acceptor leads to an overall molecular shape similar to that of substituted purines. There is a marked propensity for these nitroso compounds to crystallize with Z′ = 2. The structure of an analogue with no nitroso group is also reported for comparative purposes. Compounds containing the N-alkyl substituents —NHCH2COOEt, —NHCH2CH2COOEt and —NHCH(CH2Ph)COOEt, derived from amino acid esters, exhibit a rich variety of conformational behaviour, and in all of the nitroso compounds the bond lengths provide strong evidence for a highly polarized electronic structure. Associated with this polarization is extensive charge-assisted hydrogen bonding between the molecules, leading to supramolecular aggregation in the form of finite (zero-dimensional) aggregates, chains, molecular ladders, sheets and frameworks.

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47

Grüner, Bohumír, Bernard Bonnetot, and Henri Mongeot. "Synthesis of N- and B-Substituted Derivatives of closo-Amino-undecahydro-dodecaborate(1-) Anion." Collection of Czechoslovak Chemical Communications 62, no. 8 (1997): 1185–204. http://dx.doi.org/10.1135/cccc19971185.

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The synthesis of nitrogen and boron substituted derivatives of the 1-amino-closo-dodecaborate anion(1-) 1 is reported. Reasonable yields of the [R2NH-B12H11]- derivatives (R = C6H5CH2, 2-C10H7CH2, n-C16H33, n-C12H25) were obtained via conventional alkylation of 1 in aqueous propan-2-ol, starting from bulky primary alkylhalides. These [R2NH-B12H11]- derivatives were subsequently methylated by dimethyl sulfate under similar conditions. Reaction of 1 with palmitoyl chloride gave under anhydrous conditions the corresponding N-acyl derivative. Reaction of 1 with hydroxymethyl-18-crown-6 tosylate in THF in the presence of NaH led to the novel [(18-crown-6-CH2)2NH-B12H11]- anion, the Cs+ salt of which exhibits unusual solubility properties. A direct cyclization reaction of pentaethylene glycol ditosylate with 1 gave under similar conditions [(15-azacrown)-5-B12H11]-, the first known closo-borate anion with an attached aza-crown ring. These species exhibit potentially interesting complexation efficiency and solubility properties. Selective substitution of the boron cage by a bulky naphthyl substituent was achieved by palladium-mediated cross-coupling reaction between 1 and 1-BrMgC10H7. All derivatives were characterized by high-field 11B, 1H NMR and negative FAB mass spectrometry methods.

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48

Saini, Sachin. "Synthesis and Anticonvulsant Studies of Thiazolidinone and Azetidinone Derivatives from Indole Moiety." Drug Research 69, no. 08 (December 20, 2018): 445–50. http://dx.doi.org/10.1055/a-0809-5098.

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Abstract2-Amino-5-(3’-indolomethylene)-1, 3 , 4 - oxadiazole (3) undergoes facile condensation with various aromatic aldehydes to gave 2-substitiuted arylidenylamino-5-(3’- indolomethylene) – 1, 3 , 4 – oxadiazole (4–8). Cyclocondensation of (4–8) with thioglycolic acid and triethylamine yielded 3-[5’-(3”- indolomethylene)- 1’, 3’, 4’- oxadiazol-2’-yl]- 2- (substituted aryl)-4- thiazolidinones (9–13) and 1-[5’-(3”- indolomethylene) -1’, 3’, 4’- oxadiazol - 2’- yl ] -4-(substituted aryl) -2- azetidinones (14–18). The structures of these compounds were established on the basis of analytical and spectral data. The newly synthesised compounds were evaluated for their anticonvulsant activity and acute toxicity.

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49

El-Agrody, Ahmed M., Fathy A. Eid, Hussein A. Emam, Hany M. Mohamed, and Ahmed H. Bedair. "Synthesis of 9-Methoxy and 9-Acetoxy-3-amino-1-(4-methoxyphenyl)- 1H-benzo[f]chromene-2-carbonitriles via 2-(Imino-piperidin-1-yl-methyl)- 3-(4-methoxyphenyl)acrylonitrile as Intermediate." Zeitschrift für Naturforschung B 57, no. 5 (May 1, 2002): 579–85. http://dx.doi.org/10.1515/znb-2002-0516.

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Several new 1H-benzo[f]chromene derivatives (3aÐd) were prepared by the reaction of 7-substituted-2-naphthols (1a,b) with substituted α-cyano-4-methoxycinnamonitriles (2a,b) together with 2-(imino-piperidin-1-yl-methyl)-3-(4-methoxyphenyl)acrylonitrile (4) as intermediate. Also, the reaction of 1a,b with 4 without catalyst afforded 9-methoxy and 9-acetoxy- 3-amino-1-(p-methoxyphenyl)-1H-benzo[f]chromene-2-carbonitrile (3b,e). The reaction of 3a,b with different electrophilic and nucleophilic reagents afforded the 12H-7-oxa-8,10-diazabenzo[ a]anthracene derivatives 5, 9, 10 and 1H-benzo[f]chromene derivatives 6Ð8, 11.

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50

Mandhadi, Jithendar R., Theivendren Panneerselvam, and Pavadai Parasuraman. "DESIGN, In silico Modeling, Toxicity study and Synthesis of Novel Substituted Semicarbazide Derivatives of Pyrimidine: An Antitubercular Agent." Current Bioactive Compounds 16, no. 3 (June 10, 2020): 294–301. http://dx.doi.org/10.2174/1573407214666181001112601.

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Background: A series of 1-(2-(2-amino-5-carbamoyl-6-(1-(substitutedphenyl) prop-1-enyl) pyrimidin-4-yloxy)acetyl) semicarbazide (4a-i) derivatives was synthesized from substituted aromatic aldehydes, ethyl cyanoacetate and guanidine hydrochloride and characterized by analytical and spectral data, FTIR, 1H-NMR and Mass spectroscopy data. Methods: The antiTB action of the synthesized compounds was screened in comparison with the standard drug Rifampicin using MABA assay method. The SAR of substituted aromatic aldehydes with modification at ortho, meta and para positions with electron withdrawing group. Results: The compounds 1-(2-(2-amino-5- carbamoyl-6-(1-(2-fluorophenyl) prop-1-enyl) pyrimidin-4- yloxy) acetyl) semicarbazide and 1-(2-(2-amino- 5-carbamoyl-6-(1-(3-chlorophenyl) prop-1-enyl) pyrimidin-4-yloxy) acetyl) semicarbazide showed equal MIC values against Mycobacterium tuberculosis H37Ra with the value of 3.90μg/ml. Conclusion: The SAR study revealed that the antiTB activity of the synthesized compounds were affected by lipophilicity of the substituent.

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