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Full-Text Articles in Physical Sciences and Mathematics
Synthesis, Biological Evaluation, And In Silico Study Of Some Unique Multifunctional 1,2,4-Triazole Acetamides, Almas Sattar, Aziz Ur Rehman, Muhammad Athar Abbasi, Sabahat Zahra Saddiqui, Shahid Rasool, Hira Khalid, Muhammad Arif Lodhi, Farman Ali Khan
Synthesis, Biological Evaluation, And In Silico Study Of Some Unique Multifunctional 1,2,4-Triazole Acetamides, Almas Sattar, Aziz Ur Rehman, Muhammad Athar Abbasi, Sabahat Zahra Saddiqui, Shahid Rasool, Hira Khalid, Muhammad Arif Lodhi, Farman Ali Khan
Turkish Journal of Chemistry
The imperative demand for antibacterial agents and enzyme inhibitors prompted us to synthesize some new compounds, 6a-6k, bearing multifunctional moieties. The target acetamides were derived from 4-phenyl-5-(1-tosylpiperidin-4-yl)-4$H$-1,2,4-triazole-3-thiol (3). The structural analysis was carried out using modern spectroscopic techniques including IR, NMR, and EIMS spectral analysis. The antibacterial activity was screened against five bacterial strains including three gram-negative and two gram-positive ones. Enzyme inhibition was carried out against lipoxygenase enzyme and results were supported by in silico study. The synthesized compounds were proved to be potent antibacterial agents and enzyme inhibitors.
$S$-Substituted Derivatives Of 1,2,4-Triazol-3-Thiol As New Drug Candidates For Type Ii Diabetes, Aziz Ur Rehman, Khadija Nafeesa, Muhammad Athar Abbasi, Sabahat Zahra Saddiqui, Shahid Rasool, Syed Adnan Ali Shah, Muhammad Ashraf, Muhammad Arif Lodhi, Farman Ali Khan, Bakht Jahan
$S$-Substituted Derivatives Of 1,2,4-Triazol-3-Thiol As New Drug Candidates For Type Ii Diabetes, Aziz Ur Rehman, Khadija Nafeesa, Muhammad Athar Abbasi, Sabahat Zahra Saddiqui, Shahid Rasool, Syed Adnan Ali Shah, Muhammad Ashraf, Muhammad Arif Lodhi, Farman Ali Khan, Bakht Jahan
Turkish Journal of Chemistry
The therapeutic applications of 1,2,4-triazoles motivated us to synthesize some new derivatives. Two series of $S$-substituted derivatives (8a-8j, 12a-12i) of 5-$\{$1-[(4-chlorophenyl)sulfonyl]-3-piperidinyl$\}$-4-phenyl-4$H$-1,2,4-triazol-3-thiol (6) have been synthesized and evaluated for their biological potential. Using 4-chlorobenzene sulfonyl chloride (1) and ethyl piperidine-3-carboxylate (2), ethyl 1-[(4-chlorophenyl)sulfonyl]piperidine-3-carboxylate (3) was synthesized and converted into 3,4,5-trisubstituted 1,2,4-triazole (6) through formation of the corresponding carbohydrazide (4) and hydrazinecarbothioamide (5). Compound 6 was transformed into 8a-8j by alkyl halides (7a-7j) and into 12a-12i by $N$-aralkyl/aryl-2-bromoacetamides (11a-11i) in an aprotic solvent. The electrophiles, 11a-11i, were synthesized by gearing up $N$-substituted aralkyl/aryl amines (10a-10i) with 2-bromoacetyl bromide (9) under dynamic pH …
Synthesis And Antimicrobial And Antioxidant Activities Of Hybrid Molecules Containing Benzotriazole And 1,2,4-Triazole, Mahesh Chand, Reena Kaushik, Subhash Chand Jain
Synthesis And Antimicrobial And Antioxidant Activities Of Hybrid Molecules Containing Benzotriazole And 1,2,4-Triazole, Mahesh Chand, Reena Kaushik, Subhash Chand Jain
Turkish Journal of Chemistry
Eleven novel 1,2,4-triazolylbenzotriazoles have been prepared using 1-(hydrazinylcarbonylmethyl)-1$H$-benzot- riazole (3) as a potent intermediate. Compound 3, however, was obtained from benzotriazole in two steps. All synthesized compounds were characterized by detailed spectral studies like IR, $^{1}$H NMR, $^{13}$C NMR, and mass spectrometry. All synthesized compounds were evaluated for their \textit{in vitro} antimicrobial activity against seven strains of bacteria and four strains of fungi. Compounds 13, 17, 19, 20, and 21}were found to possess antibacterial activity comparable to that of ciprofloxacin against a Klebsiella pneumoniae strain. Except for compounds2 and 13, all compounds showed good antifungal activity against an Aspergillus niger …
Synthesis Of Acetamide Derivatives Of 1,2,4-Triazole Bearing Azinane And Their Binding Interactions With Bovine Serum Albumin Using Spectroscopic Techniques, Javed Iqbal, Aziz Ur Rehman, Muhammad Athar Abbasi, Sabahat Zahra Siddiqui, Hira Khalid, Sabina Jhaumeer Laulloo, Nausheen Joondan, Aniisah Banu Taupass, Shahid Rasool, Syed Adnan Ali Shah
Synthesis Of Acetamide Derivatives Of 1,2,4-Triazole Bearing Azinane And Their Binding Interactions With Bovine Serum Albumin Using Spectroscopic Techniques, Javed Iqbal, Aziz Ur Rehman, Muhammad Athar Abbasi, Sabahat Zahra Siddiqui, Hira Khalid, Sabina Jhaumeer Laulloo, Nausheen Joondan, Aniisah Banu Taupass, Shahid Rasool, Syed Adnan Ali Shah
Turkish Journal of Chemistry
A new series of acetamide derivatives containing 1,2,4-triazole and azinane moieties has been synthesized and characterized using $^{1}$H NMR, $^{13}$C NMR, IR, and EI-MS spectroscopic analysis. The intermediate triazole was synthesized through a sequential synthesis of carboxylate and carbohydrazide. The bovine serum albumin (BSA) binding of the newly synthesized 1,2,4-triazole derivatives was evaluated along with thermodynamics, site-selective binding, and synchronous study. The results obtained by BSA binding as well as thermodynamic studies justify that all the compounds show spontaneous interaction with BSA and could be effectively distributed and eliminated from the body. Therefore, the triazole-based analogs might be a useful …