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Journal articles on the topic 'Phenyl compounds – Derivatives'

Author: Grafiati

Published: 4 June 2021

Last updated: 17 February 2022

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1

Athraa H Mekky and Sajida M Thamir. "Synthesis, characterisation and antibacterial evaluation of some novel 1-phenyl-1h-tetrazole-5-thiol derivatives." International Journal of Research in Pharmaceutical Sciences 10, no. 2 (2019): 1136–42. http://dx.doi.org/10.26452/ijrps.v10i2.394.

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The aim of the study is to synthesise and. Characterize — some novel, "tetrazole., -5-thiol” derivatives. Firstly, the “1-phenyl-1H7-tetrazole-5-thiol” (A1) has been., synthesised by the reaction of phenylisothiocyanate with NaN3 in water as a solvent. Secondly, the tetrazole-5-thiol derivatives (A2-A4) were synthesised by the alkylation reaction of the compound (A1) with chloroacetone, phenacyl bromide and chloromethyl acetate respectively. The resulted percentage yield was relatively high (92%, %95, %90 respectively). Compound (A5) was synthesised by the reaction of ethyl acetate tetrazole d

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2

Farah Smaysem and Ahmed Salim. "Synthesis and Characterization of Some Heterocyclic Compounds and Evaluation of Antibacterial Activity." International Journal of Research in Pharmaceutical Sciences 11, SPL4 (2020): 2068–78. http://dx.doi.org/10.26452/ijrps.v11ispl4.4421.

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In this study, heterocyclic compounds with two nitrogen atoms are prepared by reaction of 2-aminobenzimidazole with formic acid to get amide derivatives (A), reacts with phenylhydrazine to get phenyl hydrazone derivatives (B), reacts with ethyl chloroacetate to obtain ethyl acetate derivatives (C). The derivative (D) obtains on heating in a basic medium. The (B) reacts with 2-chloroacetyl chloride to give derivatives (E). A number of Schiff bases are prepared (F, I) from reacting 2-aminobenzimidazole with benzaldehyde derivatives. The(F) reacts with propargyl bromide to give propargyl bromide

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3

A. Abdulqader, Kany, Ahmed W. Naser, Muthanna S. Farhan та Sabah J. Salih. "Synthesis, Characterization and Cytotoxic Activity of some new 1,2,3-Triazole, Oxadiazole and Aza- β-lactam Derivatives". Oriental Journal of Chemistry 34, № 5 (2018): 2350–60. http://dx.doi.org/10.13005/ojc/340516.

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A series of 1,2,3-triazole, oxadiazole and aza-β-lactam derivatives were synthesized through consecutive reaction began from o-(N-propargyl) sulfonamido benzoic acid (1a). The reaction of (1a) with absolute ethanol in the presence of concentrated H2SO4 resulted in the formation of ester derivative (2a). The product of the previous reaction was reacted with 80% hydrazine hydrate to prepare benzohydrazide derivative (3a). 1,3,4-oxadiazole compound (4a) was obtained by condensation of compound (3a) with CS2 in presence KOH . Compound (3a) react with Phenyl isocyanates to give Carboxamide derivati

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4

Danilenko, Nadezhda, Vladimir Shmalyuk, and Andrei Khlebnikov. "2-(2-(Fluorosulfonyloxy)phenyl)benzoxazole." Molbank 2021, no. 3 (2021): M1242. http://dx.doi.org/10.3390/m1242.

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The fluorosulfate derivatives of benzoxazole attract attention since benzoxazole-based compounds have a wide range of biological activities, and the ability of the –SO2F group to react with various functional groups makes it possible to synthesize various new derivatives. The new 2-(2-(fluorosulfonyloxy)phenyl)benzoxazole (2) has been synthesized by the SuFEx click reaction in a two-chamber reactor. Compound 2 is the first example of a benzoxazole derivative with a fluorosulfate-containing substituent at position two of the benzoxazole heterocycle. The anti-cancer potency of 2 was evaluated in

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5

Erdem, Ahmet, Hasan Genc, Nejdet Sen, Rafet Kilincarslan, and Emin Erdem. "The Synthesis and Reactions of Novel Pyrazole Derivatives by 4-phenylcarbonyl-5-phenyl-2,3-dihydro-2,3-furandione Reacted with Some Hydrazones." Revista de Chimie 68, no. 1 (2017): 143–46. http://dx.doi.org/10.37358/rc.17.1.5407.

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We report some novel pyrazole derivatives taking 4-phenylcarbonyl-5-phenyl-2,3-dihydro-2,3-furandione, 1. For this, 4-phenylcarbonyl-5-phenyl-2,3-dihydro-2,3-furandione, 1 was reacted with benzaldehyde(2- or 4-fluorophenyl)hydrazone to give 4-benzoyl-1-(2- or 4-fluorophenyl)-5-phenyl-1H-pyrazole-3-carboxylic acid 2a,b. Pyrazol derivative containing 2-fluorophenyl group 2a was converted into carboxylic chloride derivative 3a by thionyl chloride and then the compound 4a was obtained from reaction ammonia with compound 3a. In the next step, 4-benzoyl-1-(2-fluorophenyl)-5-phenyl-1H-pyrazole-3-carb

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6

Hishmat, O. H., S. S. Mabrouk, A. M. M. Nasef, N. M. A. Shayeb, and S. A. Ismail. "Derivatives of Khellinonequinone and their Aflatoxigenic Activity." Zeitschrift für Naturforschung B 43, no. 3 (1988): 343–46. http://dx.doi.org/10.1515/znb-1988-0318.

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Nitration of khellinone leads to the formation of a small amount of 3-nitrokhellinone and 5-acetyl-6-hydroxybenzofuran-4.7-dione (khellinonequinone) as a main product. The latter compound reacts with primary amines to give the corresponding imino compounds. Reaction of khellinone with o-phenylenediamine involves condensation followed by cyclisation. While on the other hand treating with phenyl hydrazines gives the phenyl hydrazone. The pyrazolobenzofuran derivative was obtained by the action of hydrazine hydrate on khellinonequinone. Finally the reaction with malononitrile leads to the formati

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7

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 - py

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8

Yoon, Goo, Seung Hoon Cheon, Jung Hyun Shim, and Seung Sik Cho. "Design and Evaluation of Licochalcone A Derivatives as Anticancer Agents." Natural Product Communications 13, no. 6 (2018): 1934578X1801300. http://dx.doi.org/10.1177/1934578x1801300609.

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New derivatives of licochalcone A were synthesized and evaluated for their potential anticancer activities. Compounds 6 (( E)-N-(4-(3-(5-bromo-4-hydroxy-2-methoxy phenyl) acryloyl) phenyl)-4-isopropylbenzamide) and 8 (1-(3-dimethylamino-phenyl)-3-(2-trifluoromethyl-phenyl)-propenone) showed potent activity against the screened cancer cell lines with that of compound 6 ranging from 6.9 ± 0.2 μM to 22.9 ± 3.1 μM, and that of compound 8 from 4.2 ± 0.5 μM to 11.8 ± 0.7 μM. Both compounds showed stronger cytotoxicity than that of licochalcone A. These two candidates have very different substituents

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9

Ho, Boon Kui, Zainab Ngaini, Paul Matthew Neilsen, et al. "Synthesis and Anticancer Activities of 4-[(Halophenyl)diazenyl]phenol and 4-[(Halophenyl)diazenyl]phenyl Aspirinate Derivatives against Nasopharyngeal Cancer Cell Lines." Journal of Chemistry 2017 (2017): 1–7. http://dx.doi.org/10.1155/2017/6760413.

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Aspirin and azo derivatives have been widely studied and have drawn considerable attention due to diverse biological activities. In this study, a series of 4-[(halophenyl)diazenyl]phenyl aspirinate derivatives were synthesized from the reaction of aspirin with 4-[(halophenyl)diazenyl]phenol via esterification, in the presence of DCC/DMAP in DCM with overall yield of 45–54%. 4-[(Halophenyl)diazenyl]phenol was prepared prior to esterification from coupling reaction of aniline derivatives and phenol in basic solution. All compounds were characterized using elemental analysis, FTIR, and 1H and 13C

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10

Hafez, Hend N., and Abdel-Rahman B. A. El-Gazzar. "Synthesis of Novel Pyridine Bearing Biologically Active Imidiazolyl, Pyrazolyl, Oxa/thiadiazolyl and Urea Derivatives as Promising Anticancer Agents." Current Organic Synthesis 17, no. 1 (2020): 55–64. http://dx.doi.org/10.2174/1570179417666191223163225.

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Background: A novel series of pyridine containing 1,3,4-oxa/thiadiazol derivatives 4a,b, pyrazole derivatives 5-7, thiazole derivatives 9a,b and 17a-c, urea derivatives 12a-c, imidiazole derivative 16, imidazo[1,2-a]pyridine derivatives 18a, b, tetrazole 19, pyrane 20 and pyridine derivatives 21 has been synthesized. Objective: This research aims to synthesize 6-(Trifluoromethyl)-2-[3-(trifluoromethyl)phenyl] amino nicotinohydrazide 2 and 6-(trifluoromethyl)-2-[3-(trifluoromethyl)phenyl]amino pyridin-3-carboaldhyde 15 as key intermediate for the synthesis of novel pyridine derivatives bearing

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11

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

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12

Rahman Badal, Md Mizanur, Md Tarikul Islam, Reshma Parvin, et al. "Antimicrobial, Structure-Activity Relationship and Computational Studies of Some Synthesized Chalcone Derivatives." Asian Journal of Chemistry 33, no. 3 (2021): 644–50. http://dx.doi.org/10.14233/ajchem.2021.23028.

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Several chalcones viz. 1,3-diaryl-2-propane-1-one (1a), 3-(4-hydroxy phenyl)-1-phenyl-2-propane-1- one (1b), 3-(4-amino-phenyl)-1-phenyl-2-propane-1-one (1c) and their derivatives 2-ethoxy-4,6- diphenyl-4H-pyran-3-carboxylic acid ethyl ester (2a), 4-(4-hydroxy-phenyl)-7,7-dimethyl-2-phenyl- 4,6,7,8-tetrahydro-chromen-5-one (2b) and 7-(4-amino-phenyl)-5-phenyl-1,5-dihydropyrano[2,3- d]pyrimidine-2,4-dione (2c ) have been synthesized following both conventional and microwave irradiation methods. The structures of the isolated compounds were elucidated on the basis of UV-visible, FTIR, 1H NMR spe

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13

Journal, Baghdad Science. "Synthesis of Some Heterocyclic Compounds Derived from 2-Mercapto Benzoxazole." Baghdad Science Journal 10, no. 3 (2013): 766–78. http://dx.doi.org/10.21123/bsj.10.3.766-778.

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New series of 2-mecapto benzoxazole derivatives (1-20) incorporated into fused to different nitrogen and suphur containing heterocyclic were prepared from 2-meracpto benzoxazole, when treated with hydrazine hydrate to afford 2-hydrazino benzoxazol (1). Compound (1) converted to a variety of pyridazinone andphthalazinone derivatives (2-4) by reaction with different carboxylic anhydride. Also, reaction of (1) with phenyl isothiocyanate and ethyl chloro acetate afforded 3-phenyl-1,3-thiazolidin-2,4-dione-2-(benzoxazole-2-yl-hydrazone) (6). Azomethines (7-10) were prepared through reaction of (1)

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14

Lahsasni, Siham, Dunya A. M. Al-Hemyari, Hazem A. Ghabbour, et al. "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,

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15

Hayun, H., R. N. Fauzan, N. T. Wibowo, A. Asrianingtiyas, N. Afriliana, and T. Ananda. "Synthesis and Anti-inflammatory Activity of 2-Methoxy-4-(1-phenyl-3- methyl-1H-pyrazol-5-yl)phenol) and Its Aminomethyl Derivatives." Asian Journal of Chemistry 32, no. 3 (2020): 607–11. http://dx.doi.org/10.14233/ajchem.2020.22159.

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Using heat-induced protein denaturation technique, a series of novel synthesized 1,5-diarylpyrazole compounds, namely 2-methoxy-4-(1-phenyl-3-methyl-1H-pyrazol-5-yl)phenol (1) and its aminomethyl derivatives (2a-e) were evaluated for their anti-inflammatory potentiality. The structures of the synthesized compounds were elucidated using FTIR, NMR (1H & 13C) and mass spectral data. The study found that the activity of aminomethyl derivatives (2a-e) was higher than that of parent compound 1. In this series, aminomethyl derivatives bearing dimethylamino-methyl, diethylaminomethyl and pyrrolidi

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16

Hafez, Hend N., Abdel-Rhman B. A. El-Gazzar, and Magdi E. A. Zaki. "Simple approach to thieno[3,2-d]pyrimidines as new scaffolds of antimicrobial activities." Acta Pharmaceutica 66, no. 3 (2016): 331–51. http://dx.doi.org/10.1515/acph-2016-0029.

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Abstract 6ʹ-(4-Chlorophenyl)-spiro[cyclohexane-1,2ʹ-thieno[3,2-d][1,3] oxazin]-4ʹ(1ʹH)-one (1) was synthesized and used as a starting material for the synthesis of a novel series of spiro compounds having biologically active sulfonamide 2a-e and 3ʹ-(4-acetylphenyl)-6ʹ- (4-chlorophenyl)-1ʹH-spiro[cyclohexane-1,2ʹ-thieno[3,2-d] pyrimidine-4ʹ(3ʹH)-one (3). Compound 2a was used as a key intermediate for the synthesis of sulfonyl carbothioamide derivatives 4a-c. Also, compound 3 was used as an intermediate for the synthesis of 3ʹH-spiro[cyclohexane-1,2ʹ-thieno[3,2-d]pyrimidin]-3ʹ-yl] phenyl}-2-imin

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17

Deli, József, Tamás Lóránd, Dezsö Szabó, András Földesi, and Adolf Zschunke. "Synthesis of 2-amino-8-benzylidene-4-phenyl-3,4,5,6,7,8-hexahydro- and -5,6,7,8-tetrahydroquinazoline derivatives." Collection of Czechoslovak Chemical Communications 50, no. 7 (1985): 1602–10. http://dx.doi.org/10.1135/cccc19851602.

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Base-catalyzed reaction of 2,6-dibenzylidenecyclohexanone and alkylguanidines gave 2-alkylamino-8-benzylidene-4-phenyl-3,4,5,6,7,8-hexahydroquinazolines IVa-c, which were oxidized to 2-alkylamino-8-benzylidene-4-phenyl-5,6,7,8-tetrahydroquinazolines Va-c. The acylamino (VIa-c, VIIa-d, IXa,b) and diacylamino derivatives (VIIIa,b) of the 2-amino-8-benzylidene-4-pheny]-3,4,5,6,7,8-hexahydroquinazoline (II), 2-amino-8-benzylidene-4-phenyl-5,6,7,8-tetrahydroquinazoline (III) and compounds Va-c have also been prepared. These compounds having the E-configuration were converted into the Z isomers XIIa

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18

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

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19

Mehta, Prakash, Prakash Davadra, Nirav Shah, and Hitendra Joshi. "Synthesis and Antimicrobial Activity of Some New Imidazolinone Derivatives Containing Benzimidazole." International Letters of Chemistry, Physics and Astronomy 29 (March 2014): 74–80. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.29.74.

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In this study some new o-benzimidazol-2'-yl-benzamido-p'-benzamido-2-phenyl-4-substituted phenyl-5-oxo-Imidazolines 3a-3j were synthesized. To synthesized target molecules we used various substituted oxazolone derivatives, synthesized from substituted benzaldehyde with hippuric acid. Substituted oxazolones 2a-2j were reacted with carbohydrazide derivative of benzimidazole 1 in presence of pyridine as base to obtained substituted imidazolinone derivatives. All synthesized compounds were characterized by IR, 1H NMR, elemental analysis and further supported by mass spectroscopy. All synthesized c

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20

Rao, Nalla Krishna, Tentu Nageswara Rao, Botsa Parvatamma, Y. Prashanthi, and Ravi Kumar Cheedarala. "Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihydroisoquinoline-2(1H)-yl)methyl) oxazol-5(4H)-one Derivatives Using 1,2,3,Tetrahydroisoquinoline and their Antimicrobial Activity." Current Organic Synthesis 17, no. 5 (2020): 396–403. http://dx.doi.org/10.2174/1570179417666200415151228.

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Aims: A series of six 4-benzylidene-2-((1-phenyl-3,4-dihydro isoquinoline-2(1H)-yl)methyloxazol- 5(4H)-one derivatives were synthesized by condensation of substituted aryl aldehydes with 2-(2-(1-phenyl-3,4- dihydro isoquinoline-2(1H)-acetamido)acetic acid in the presence of sodium acetate, acetic anhydride and zinc oxide as catalysts. Background: Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihy droisoquinoline-2(1H)-yl)methyl)oxazol- 5(4H)-one derivatives using 1,2,3,Tetrahydroisoquinoline and their antimicrobial activity. Objective: The title compounds can be synthesized from 1,2,3,4-te

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21

Journal, Baghdad Science. "Synthesis of New Heterocyclic Derivatives from 4-(3, 5-Dimethyl-1-phenyl-1H-pyrazol-4-ylazo)- benzoic acid." Baghdad Science Journal 7, no. 1 (2010): 727–36. http://dx.doi.org/10.21123/bsj.7.1.727-736.

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In this work pyrazolin derivatives were prepared from the diazonium chloride salt of 4-aminobenzoic acid. Azo compounds were prepared from the reaction of an ethanolic solution of sodium acetate and calculated amount of active methylene compound namely, acetyl acetone to obtain the corresponding hydrazono derivative (1). Cyclocondensation reaction of compounds (1) with hydrazine hydrate and phenyl hydrazine in boiling ethanol affording the corresponding pyrazoline-5-one derivatives of 4-aminobenzoic acid (2,3). Then compound (3) was reacted with thionyl chloride to give the corresponding acid

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22

Garozzo, Adriana, Christian CC Cutri, Christophe Pannecouque, Angelo Castro, Francesco Guerrera, and Erik De Clercq. "Isothiazole Derivatives as Antiviral Agents." Antiviral Chemistry and Chemotherapy 18, no. 5 (2007): 277–83. http://dx.doi.org/10.1177/095632020701800503.

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We recently described the synthesis and antiviral activity of the compounds 5-phenyl-3-(4-cyano-5-phenylisothiazol-3-yl) disulphanyl-4-isothiazole-carbonitrile and S-(4-cyano-5-phenylisothiazol-3-yl)- O-ethyl thiocarbonate, which were found to be effective against both HIV-1 (IIIB) and HIV-2 (ROD). We have now evaluated these compounds against both RNA and DNA viruses, obtaining high selectivity indexes for poliovirus 1 (SI: 223 and 828, respectively) and Echovirus 9 (SI: 334 and 200, respectively). In our previous studies, 3-methylthio-5-(4- OBn-phenyl)-4-isothiazolecarbo-nitrile was found to

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23

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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24

Morshed, MH, MF Islam, MA Yousuf, GMG Hossain, JA Khanam, and MA Salam. "Synthesis and Antimicrobial Screening of Three Triazole Derivatives." Dhaka University Journal of Pharmaceutical Sciences 10, no. 1 (2012): 43–47. http://dx.doi.org/10.3329/dujps.v10i1.10014.

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Due to the medicinal importance of triazole derivatives, the antimicrobial property of three synthesized triazole derivatives were screened in vitro against some Gram positive and Gram negative pathogenic bacteria and some pathogenic fungi. In this study, three compounds 2-(5-mercapto-4-phenyl-4H-[1,2,4] triazole-3-yl]-cyclohexa- 1,5-dienol (S1), 2-[5-mercapto-4-(2-mercapto-phenyl)-4H- [1,2,4] triazole-3-yl]-phenol (S2) and 4-[3-(2-hydroxyphenyl)- 5-mercapto-[1,2,4] triazole-4-yl]-benzene sulfonamide (S3) have been synthesized. The minimum inhibitory concentration (MIC) and the minimum bacteri

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25

Cherala, Swapna, Harikiran Lingabathula, Rama Ganta, Srinivas Ampati, and Sarangapani Manda. "Synthesis and Anti-Inflammatory Activity of a Novel Series of Diphenyl-1,2,4-triazoles and Related Derivatives." E-Journal of Chemistry 9, no. 4 (2012): 2510–15. http://dx.doi.org/10.1155/2012/278695.

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In the present investigation we have synthesized a series of new 1-[3-(4-substitutedphenyl)-5-phenyl-4H-1,2,4-triazol-4-yl]urea and 1-[3-(4-substitutedphenyl)-5-phenyl-4H-1,2,4-triazol-4-yl]thiourea derivatives (4Ia - 4IId). The newly synthesised derivatives were characterized by using the data of IR,1H NMR and Mass Spectral analysis. Thus synthesised and characterized targetted compounds were further screened for their anti-inflammatory activity by using Carrageenan – induced paw edema rat model. Among all the newly synthesized derivatives, Compounds 4Ia-4Ic and Compounds 4IIa-4IId were reduc

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26

da Silva Lima, Camilo Henrique, Júlio César de Araujo Vanelis Soares, Joana Lucius de Sousa Ribeiro, Estela Maris Freitas Muri, Sérgio de Albuquerque, and Luiza Rosaria Sousa Dias. "Anti-Trypanosoma cruzi Activity and Molecular Docking Studies of 1Hpyrazolo[ 3, 4-b]pyridine Derivatives." Letters in Drug Design & Discovery 17, no. 2 (2020): 184–91. http://dx.doi.org/10.2174/1570180816666190305141733.

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Background: Untargeted studies led to the development of some pyrazolopyridine derivatives for the antiparasitic profile, particularly the derivatives containing the structural carbohydrazide subunit. In this work, we proceeded in the biological screening of 27 N’- (substitutedphenylmethylene)- 4-carbohydrazide-3-methyl-1-phenyl-1H-pyrazolo[3, 4-b]pyridine derivatives against T. cruzi as well as the cytotoxic evaluation. To obtain more information about the trypanocidal activity of this class of compounds, we carried out molecular docking simulations to get an insight into putative targets in

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27

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 (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 deriv

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28

Ozer, Erdem Kamil, Miyase Gozde Gunduz, Ahmed El-Khouly, et al. "Synthesis of fused 1,4-dihydropyridines as potential calcium channel blockers." Turkish Journal of Biochemistry 43, no. 6 (2017): 578–86. http://dx.doi.org/10.1515/tjb-2016-0247.

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AbstractObjectiveThe aim of this study was to synthesize ten 1,4-dihydropyridine (DHP) derivatives in which substituted cyclohexane rings were fused to the DHP ring and to determine how different ester groups and the benzoyl substituent introduced in 4-phenyl ring affected their calcium channel blocking activity.MethodsA microwave-assisted one-pot method was applied for the synthesis of compound1–5according to a modified Hantzsch reaction. The benzoyl moiety was introduced in the 4-phenyl ring of these dihydropyridines by refluxing with benzoyl chloride in acetone in the presence of anhydrous

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29

Hafez, Hend N., and Abdel-Rhman B. A. El-Gazzar. "Synthesis and evaluation of antitumor activity of new 4-substituted thieno[3,2-d]pyrimidine and thienotriazolopyrimidine derivatives." Acta Pharmaceutica 67, no. 4 (2017): 527–42. http://dx.doi.org/10.1515/acph-2017-0039.

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Abstract 3-Methyl-6-phenyl-2-thioxo-2,3-dihydrothieno[3,2-d]pyrimidin- 4(1H)-one (2), on treatment with phosphorous oxychoride, affored 4-chloro-3-methyl-6-phenyl -thieno[3,2-d]pyrimidine- 2(3H)-thione (3). A series of novel 6-phenyl-thieno[3,2-d]pyrimidine derivatives 4-9 bearing different functional groups were synthesized via treatment of compound 3 with different reagents. On the other hand, compound 2 was used to synthesize ethyl-[(3-methyl-6-phenyl-2-thioxo-2,3-dihydrothieno[ 3,2-d]pyrimidin-4-yl)-oxy]acetate (10), 2-hydrazinyl- -3-methyl-6-phenyl-thieno[3,2-d]pyrimidin-4(3H)-one (11), 3

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30

Amr, Abdel-Galil E. "Synthesis of Some New Linear and Chiral Macrocyclic Pyridine Carbazides as Analgesic and Anticonvulsant Agents." Zeitschrift für Naturforschung B 60, no. 9 (2005): 990–98. http://dx.doi.org/10.1515/znb-2005-0914.

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A series of 2,6-disubstituted pyridine derivatives were prepared from 2,6-diacetylpyridine or 2,6- dicarbonyl pyridine dichloride as starting materials. Reaction of 2,6-diacetylpyridine 1 with hydroxylamine hydrochloride or different aromatic aldehydes afforded the corresponding 2,6-diacetylpyridine dioxime and 2,6-bis-[β -(2-thienyl)acryloyl]pyridine derivatives 2 and 3, respectively. Additionally, N2,N2‘-(pyridine-2,6-dicarbonyl)-L-amino acid hydrazides 5 were prepared starting from 2,6- dicarbonyl pyridine dichloride via the corresponding esters 4. Compound 3 was reacted with hydroxylamine

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31

Janam Singh, Ram, and Dharmendra Kumar Singh. "Syntheses of Some 3,5-Diaryl-4H-1,2,4-triazole Derivatives and their Antifungal Activity." E-Journal of Chemistry 6, s1 (2009): S219—S224. http://dx.doi.org/10.1155/2009/925964.

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Syntheses of a series of 3, 5-diaryl-4H-1, 2, 4-triazole derivatives are described. In this present work, 4-amino-3-phenyl-5-p-tolyl-4H-1,2,4-triazole(1) was converted toN,N’-bis[3-phenyl-5-p-tolyl-4H-1,2,4-triazolyl]-1,4-xylenediimine(2) and 3-Phenyl-5-p-tolyl-4-[4-methyl benzylidenamino]-4H-1,2,4-triazole (3) in good yields by treatment with aldehydes OHC-C6H4-CHO and Ar-CHO respectively. The compoundsN,N’-bis[3-phenyl-5-p-tolyl-4H-1,2,4-triazolyl]-1,4-xylenediimine (2) and 3-phenyl-5-p-tolyl-4-[4-methyl benzylidenamino]-4H-1,2,4-triazole (3) were reduced with NaBH4to afford the correspondin

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32

Hashem, Heba E., and Ahmed M. Abo-Bakr. "Synthesis of Some New 1,2,4-Triazine and 1,2,5-Oxadiazine Derivatives with Antimicrobial Activity." Heteroatom Chemistry 2019 (September 25, 2019): 1–7. http://dx.doi.org/10.1155/2019/2326514.

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1,2,4-Triazine and 1,2,5-oxadiazine derivatives 2–12 were obtained from treated 1,3-oxazolone (1) with phenyl hydrazine or hydroxylamine hydrochloride. Chlorotriazine derivative 3 undergoing condensation reactions with different reagents produced new fused tetrazolo-triazine and triazino-quinazolinone derivatives. 1,2,5-Oxadiazine has been used as a synthon for the fused pyrazolo-oxadiazine derivative. The constitution of the prepared compounds was built up based on microanalytical and spectral data. Some of the new compounds were assessed for their antimicrobial activity.

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33

Journal, Baghdad Science. "Synthesis of New Mannich Bases from Indole Derivatives." Baghdad Science Journal 9, no. 1 (2012): 168–77. http://dx.doi.org/10.21123/bsj.9.1.168-177.

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This work includes two steps of synthesis, the first one is the synthesis of indole which was prepared according to literature of the reaction of phenyl hydrazine with acetaldehyde in glacial acetic acid afforded phenyl hydrazone of acetaldehyde , this product was fused with zinc chloride to give the indole.Reaction of cyclohexanone with phenyl hydrazine using the same procedure for the preparing giving 1,2,3,4-Tetrahydrocarbazole.Second step involved synthesis of a series of (17) of mannich bases derivatives of indole and 1,2,3,4-Tetrahydrocarbazle. Mannich reaction involves the condensation

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34

Aksyonova-Seliuk, I. I., O. I. Panasenko, and E. G. Knysh. "Synthesis and structural features of 5-(4-(tert-butyl) phenyl)-4-((R)amino)-4H-1,2,4-triazole-3-thiols." Farmatsevtychnyi zhurnal, no. 6 (August 14, 2018): 60–65. http://dx.doi.org/10.32352/0367-3057.6.16.03.

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Chemistry of heterocyclic compounds is one of the most popular sector in organic chemistry. Scientists allocate among them a class of derivatives of 1,2,4-triazole. This class of compounds attracts attention his broad spectrum of biological activity. There are antiviral, anti-inflammatory, anti-tubercular, antimicrobial, antioxidant, actoprotective, anti-cancer and other activities. The derivatives of 1,2,4-triazole have one more important advantage. It is low toxicity. This properties do this class of derivatives promising for researches their chemical structure and biological activity and pu

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35

El-Sharief, Marwa A. M. Sh, Samir Y. Abbas, Medhat A. Zahran, Yehia A. Mohamed, Ahmed Ragab, and Yousry A. Ammar. "New 1,3-diaryl-5-thioxo-imidazolidin-2,4-dione derivatives: synthesis, reactions and evaluation of antibacterial and antifungal activities." Zeitschrift für Naturforschung B 71, no. 8 (2016): 875–81. http://dx.doi.org/10.1515/znb-2016-0054.

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AbstractNew cyanothioformamide derivative 1 was prepared by treatment of 3,5-dichlorophenyl isothiocyanate with potassium cyanide at room temperature. Cycloaddition of cyanothioformamide 1 with phenyl isocyanate as electrophile furnished the corresponding imidazolidine 2. Imine hydrolysis of 2 with ethanolic HCl produced the corresponding 4-thioxo-2,5-imidazolidinedione 3. This compound was used as key synthon for the preparation of a wide variety of new substituted imidazole compounds. Condensation of 3 with different types of hydrazine derivatives furnished new series of hydrazone 4a, b, thi

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36

Lu, Shan, Siegfried Draeger, Barbara Schulz, et al. "Bioactive Aromatic Derivatives from Endophytic Fungus, Cytospora sp." Natural Product Communications 6, no. 5 (2011): 1934578X1100600. http://dx.doi.org/10.1177/1934578x1100600518.

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Two new benzyl γ-butyrolactone analogues, ( R)-5-(( S)-hydroxy(phenyl)-methyl)dihydrofuran-2(3H)-one (1) and its 6-acetate (2), and a new naphthalenone derivative (8), together with eight additional known aromatic derivatives, ( S)-5-(( S)-hydroxy(phenyl)-methyl)dihydrofuran-2(3H)-one (3), ( S)-5-benzyl-dihydrofuran-2(3H)-one (4), 5-phenyl-4-oxopentanoic acid (5), γ-oxo-benzenepentanoic acid methyl ester (6), 3-(2,5-dihydro-4-hydroxy-5-oxo-3-phenyl-2-furyl)propionic acid (7), (3 R)-5-methylmellein (9), integracins A (10) and B (11) were isolated from Cytospora sp., an endophytic fungus isolate

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37

Solankee, Anjani, and Riki Tailor. "Synthesis, Characterisation and Biological Screening of s-Triazine Based Chalcones and its Derivatization into Phenyl Pyrazolines, Isoxazoles." International Letters of Chemistry, Physics and Astronomy 47 (February 2015): 109–19. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.47.109.

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Heterocyclic derivatives such as phenyl pyrazolines and isoxaxoles were prepared from s - triazine based chalcones. Chalcones (A1 - A5) are synthesised by the reaction of compound (V) with various aromatic aldehydes. Moreover, further reaction of chalcones with phenyl hydrazine hydrochloride and hydroxylamine hydrochloride in the presence of alkali gives phenyl pyrazolines (A6 - A10) and isoxazoles (A11 - A15) derivatives respectively. The structures of the newly synthesised compounds were confiremed by spectroscopic (IR, 1H NMR, 13C NMR) and elemental analysis. All the newly synthesised compo

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38

Patel, Pineshkumar N., and Denish C. Karia. "Synthesis and Antimicrobial Activity of Novel Series of Diversely Substituted Acetyl Pyrazoline Bearing Biphenyl Carbonitrile Motif." International Letters of Chemistry, Physics and Astronomy 69 (August 2016): 42–48. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.69.42.

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Novel series of diversely substituted acetyl pyrazoline having biphenyl carbonitrile motif have been synthesized. The reaction of 2-cyno-4’-bromomethyl biphenyl with1-(4-hydroxy-phenyl)-ethanone resulted in acetophenone derivative of biphenyl-2-carbonitrile. This acetophenone derivative was condensed with substituted aromatic aldehyde in mixed solvent resulted in various substituted chalcones. These chalcones were further cyclized using hydrazine hydrate in presence of glacial acetic acid to produce titled compound derivatives. The chemical structures of synthesized compounds were elucidated b

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39

Betala, Sailu, Hanumandlu Racha, and Chiranjeevi Abba. "Synthesis of Novel Triazolothione, Thiadiazole, Triazole and Oxadiazole Functionalized Tri-fluoromethylnaphthyridine Derivatives and their Anticancer Activity & Antimicrobial Activity." Asian Journal of Chemistry 32, no. 8 (2020): 1931–40. http://dx.doi.org/10.14233/ajchem.2020.22688.

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Novel triazolothione, thiadiazole, triazole and oxadiazole-tagged trifluoromethyl group containing naphthyridine derivatives (6a-l and 7a-d) were synthesized from 2-amino-6-(thiophen-2-yl)-4- (trifluoromethyl)nicotinonitrile (1) on treatment with acetophenone and obtained 2-phenyl-7-(thiophen- 2-yl)-5-(trifluoromethyl)-1,8-naphthyridin-4-amine (2), compound 2 on reaction with bromoethylacetate and after that reaction with hydrazine hydrate and obtained carbohydrazide derivatives (4), compound 4 on reaction with different substituted phenyl isothiocyanates to obtain phenyl hydrazine carbothiami

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40

Djudjic, Radana, and Branka Rodic-Grabovac. "Synthesis of dialkylaminocarbonyl N-chloro- carbonyl-N-phenyl-4-aminobenzo-(-pyrone derivatives." Acta Periodica Technologica, no. 35 (2004): 187–91. http://dx.doi.org/10.2298/apt0435187d.

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The title compounds were prepared by condensation of N-chlorocarbonyl-N-phenyl-4-aminobenzo-(-pyrone with diethylamine dibutylamine and isopropylamine. The starting compound used for condensation with amines was obtained by a reaction of N-phenyl-4-aminobenzo-(-pyrone with oxalyl chloride.

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41

Gopa, N., E. Porchezhian, and G. V. S. Rama Sarma. "ANALGESIC AND ANTI-INFLAMMATORY ACTIVITIES OF 2-PHENYL (6, 8-DISUBSTITUTED 3,4-DIHYDRO-4-OXOQUINAZLIN-3-YCL) ACETO ACETAMIDES AND THEIR ß (4-SUBSTITUTED PHENYL) AZO ANALOGS." Scientia Pharmaceutica 69, no. 1 (2001): 27–32. http://dx.doi.org/10.3797/scipharm.aut-01-04.

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2-phenyl-(3,4-dihydro-4-oxoquinazolin-3-yalc)e to acetamides (1&2) and their B-(4-substituted phenyl) azo derivatives (3-10) were evaluated for their analgesic and antiinflammatory activities. The bromophenyl azo derivative (4) showed significant activity as comparable to standard drugs viz pentazocine, aspirin and other compounds exhibited moderate activities. All the synthesized compounds were tested for their toxicity have not shown any abnormality up to 1500 mg/kg Body weight in experimental animals.

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42

Desai, S. N. Mamle, Rudrax N. S. Priolkar, Harshank A. Naik Karmali, Prabhav D. Ambe, and B. S. Biradar. "SYNTHESIS, CHARACTERIZATION AND EVALUATION OF 4-HYDROXY-1-PHENYL/METHYL-3-(3-SUBSTITUTED-1-(SUBSTITUTEDIMINO) PROPYL) QUINOLINE-2(1H)-ONE DERIVATIVES AND 4-HYDROXY-1-PHENYL/METHYL-3-(1-(SUBSTITUEDIMINO) ETHYL) QUINOLINE-2(1H)-ONE DERIVATIVES AS POSSIBLE ANTICANCER AGENTS." International Journal of Pharmacy and Pharmaceutical Sciences 9, no. 10 (2017): 240. http://dx.doi.org/10.22159/ijpps.2017v9i10.20184.

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Objective: Synthesis, characterization and evaluation of quinolin-2-one derivatives as possible anticancer agents.Methods: A series of novel 4-hydroxy-1-phenyl/methyl-3-(3-substituted-1-(substitutedimino)propyl)quinolin-2(1H)-one derivatives IIa(1-5)/IIb(1-5) and 4-hydroxy-1-phenyl/methyl-3-(1-(substituedimino)ethyl)quinolin-2(1H)-one derivatives IIIa(1-3)/IIIb(1-3) were synthesised by nucleophilic addition of substituted anilines on 3-acetyl-4-hydroxy-1-phenyl/methylquinolin-2(1H)-one (a/b) and 4-hydroxy-3-(3-substitutedpropanoyl)-1-phenyl/methyl quinolin-2(1H)-one (Ia/Ib); respectively. The

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43

Hadanu, Ruslin, Mustofa Mustofa, and Nazudin Nazudin. "Synthesis and Antimalarial Activity of 2-Phenyl-1,10-Phenanthroline Derivative Compounds." Jurnal Natur Indonesia 15, no. 1 (2014): 57. http://dx.doi.org/10.31258/jnat.15.1.57-62.

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To develop new potential antimalarial drugs of 2-phenyl-1,10-phenanthroline 5 derivatives from 8-aminoquinoline as startingmaterial were synthesized in good yields. The synthesis of 2-phenyl-1,10-phenanthroline 5 derivatives compoundswith 8-aminoquinoline 4 as starting material through three steps has been carried out. The first step of reactions is aldolcondensation of benzaldehyde 1 with acetaldehyde 2. The result of reactions is cinnamaldehyde 3 (92.14%) in the form ofyellow solid. The second step of reactions was synthesized of 2-phenyl-1,10-phenanthroline 5 (brown solid, 54.63%)through cy

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44

El-Ossaily, Y. A. B., R. M. Zaki, and S. A. Metwally. "Investigation and Synthesis of Some Novel Spiro Heterocycles Related to Indoline Moiety." Journal of Scientific Research 6, no. 2 (2014): 293–307. http://dx.doi.org/10.3329/jsr.v6i2.17590.

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Reactions of indole-2,3-dione 1 with 2-mercaptobenzimidazole, o-phenylenediamine, 2-aminophenol, 2-aminobenzothiazole, 2-aminobenzimidazole and 3-methyl-1-phenyl-2-pyrazolin-5-one were carried out to give compounds spiroindolethiazetobenzimidazole 2, spirobenzimidazole(oxazole)indoline 3a,b, benzothiazol(imidazol) iminoindolinone 4a,b and methyloxoindolylidenepyrazolone 5 respectively. Compound 5 was reacted with 2-aminophenol as well as o-phenylenediamine to give new spirooxazepine and diazepine derivatives 6a,b respectively. Reaction of 5 with nitrogen nucleophiles as well as carbon nucleoph

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45

Journal, Baghdad Science. "Synthesis of some Schiff's bases derivatives from aminoazo compounds." Baghdad Science Journal 4, no. 3 (2007): 416–19. http://dx.doi.org/10.21123/bsj.4.3.416-419.

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Reaction of,2- [( 4- amio phenyl ) diazenyl] 1,3,4- thiadiazole -5- thiol (S1) with p- chlorobenzeldehyde,3,4 – dimethoxy benzaldehyde and pyrrol-2- carbonxaldehyde gave -5- [{4-(4-chlorobenzylidene amino) phenyl} diezenyl]-1,3,4- thiadiazole-2- thiol (S2),5-[{ 4-[(3,4- dimethoxybenzyldene )amino phenyl ] diazenyl)-1,3,4- thiadiazole-2-thiol,(S3) and -5- [4-(1,H – pyrrol -2- yl- methylene)amino phenyl] diazenyl)-1,3,4- thiadiazole-2- thiol (S4) respectively as schiff's bases compounds. On the same route-2-[(4-amino-1- naphthyl ) diazenyl] -1,3,4- thiadiazole -5- thiol (S5) reacts with –p- chlo

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46

Kasimogullari, Rahmi, Belma Zengin, Makbule Maden, Samet Mert, and Cavit Kazaz. "Synthesis of new derivatives of 1-(3-amino-phenyl)-4- benzoyl-5-phenyl-1h-pyrazole-3-carboxylic acid." Journal of the Serbian Chemical Society 75, no. 12 (2010): 1625–35. http://dx.doi.org/10.2298/jsc101018135k.

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4-Benzoyl-1-(3-aminophenyl)-5-phenyl-1H-pyrazole-3- carboxylic acid (1) was synthesized according to the literature.1 2-(3- Aminophenyl)-3,4-diphenyl-2H-pyrazolo[3,4-d]pyridazin-7(6H)-one (5) was obtained by the cyclocondensation reaction of 1 with hydrazine hydrate. New pyrazole derivatives of compounds 1 and 5 were synthesized by their reaction with ?-diketones, ?-ketoesters, ?-naphthol, phenol and various other reagents. The structures of the synthesized compounds were characterized by 1H-NMR, 13C-NMR, IR and Mass spectroscopy, as well as elemental analysis.

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47

Shenvi, Suvarna, Latha Diwakar та G. Chandrasekara Reddy. "Nitro Derivatives of Naturally Occurring β-Asarone and Their Anticancer Activity". International Journal of Medicinal Chemistry 2014 (1 жовтня 2014): 1–5. http://dx.doi.org/10.1155/2014/835485.

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β-Asarone (2, 4, 5-trimethoxy-(Z)-1-propenylbenzene) was obtained from Acorus calamus. Nitration of β-asarone with AgNO2/I2 in ether yielded 1-(2, 4, 5-trimethoxy phenyl)-2-nitropropene (1) but with NaNO2/I2 in ethylene glycol obtained 1-(2, 4, 5-trimethoxy phenyl)-1-nitropropene (2). Compound 2 was prepared for the first time and characterized using IR, 1H-NMR, 13C-NMR, and GC-MS spectra and it was converted into 1-(2, 4, 5-trimethoxy) phenyl-1-propanone (3) using modified Nef reaction. Based on 1D NOESY experiments, compounds 1 and 2 have been assigned E configuration. Compounds 1 and 2 were

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48

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 screene

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49

Franchetti, P., P. Perlini, G. Abu Sheikha, et al. "Potent and Selective Inhibitors of Human Immunodeficiency Virus Protease Structurally Related to L-694,746." Antiviral Chemistry and Chemotherapy 9, no. 4 (1998): 21–27. http://dx.doi.org/10.1177/095632029800900402.

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A series of human immunodeficiency virus (HIV) protease inhibitors, which are analogues of N-[2( R)-hydroxy-1( S)-indanyl]-5( S)-[( tert-butyloxycarbonyl)amino]-4( S)-hydroxy-6-phenyl-2-( R)-[[4-(carboxymethoxy)phenyl]methyl]hexanamide (L-694,746), a metabolite of the anti-HIV agent L-689,502, were synthesized. In these compounds, the acetic group linked to the para position of the P1′ phenyl in the reference inhibitor was replaced either by the bioisosteric phosphonomethoxy group and its diisopropyl/dibenzyl derivatives, or the 1H-tetrazol-5-yl-methoxy group and its 1-benzyl derivative. In en

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50

Bairagi, Keshab M., Nancy S. Younis, Promise M. Emeka, et al. "Antidiabetic Activity of Dihydropyrimidine Scaffolds and Structural Insight by Single Crystal X-ray Studies." Medicinal Chemistry 16, no. 7 (2020): 996–1003. http://dx.doi.org/10.2174/1573406416666191227123048.

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Background: This research project is designed to identify the anti-diabetic effects of the newly synthesized compounds to conclude the perspective of consuming one or more of these new synthetic compounds for diabetes management. Introduction: A series of dihydropyrimidine (DHPM) derivative bearing electron releasing and electron-withdrawing substituent’s on phenyl ring (a-j) were synthesized and screened for antihyperglycemic( anti-diabetic) activity on streptozotocin (STZ) induced diabetic rat model. The newly synthesized compounds were characterized by using FT-IR, melting point, 1H and 13C

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