Synthesis Antimicrobial Screening and In Silico Studies of Novel Derivatives of 12 4 Triazole and 1 3 4 Thiadiazole

Abstract

This thesis titled Synthesis, antimicrobial screening and in silico studies of newlinenovel derivatives of 1,2,4-triazole and 1,3,4-thiadiazole was carried out to newlinesynthesize and to screen the newly developed compounds for its antimicrobial newlineactivity. Target compounds in scheme I andII were synthesized by condensing N-{4- newline[(5-sulfanyl-1,3,4-thiadiazole-2-yl)methoxy]phenyl} acetamide with N-substituted newlinechloroacetamides, and#946;-chloropropionamides, and#945;-chloropropionamides and 3-chloro-2- newlinemethylpropionamide. Schiff bases and fused thiadiazole derivatives of 4-amino-5- newline(2-chlorophenyl)-4H-1,2,4-triazole-3-thiol were synthesized in scheme III. In newlinescheme IV 4-phenyl-5-pyridin-4-yl-(4H)-1,2,4-triazole-3-thiol was condensed with newlinedifferently substitute 2-cyno-3-amino pyridine through sulphur to get the target newlinecompounds. All these synthesized compounds were characterized by satisfactory newlinephysiochemical and spectroscopic data. All the newly synthesized compounds were newlineevaluated for antibacterial activity against pathogenic gram positive bacteria newline(Staphylococcus aureus, Bacillus subtilis) and gram negative bacteria (Escherichia newlinecoli, Pseudomonas aeruginosa) using minimum inhibitory concentration (MIC) by newlinethe serial dilution method. Antifungal activity was carried out against the two fungi newlinenamely Aspergillus flavus and Candida albicans using Fluconazole as the standard newlinedrug. newlineScheme I: Among the compounds 9d, 9e, 11d and 11e bearing electron withdrawing newlinesubstituents displayed promising antibacterial and antifungal activity comparable newlinewith that of standard drug. Compound 2-(5-((4-acetamidophenoxy)methyl)-1,3,4- newlinethiadiazol-2-ylthio)-N-(4-nitrophenyl)acetamide (9e) was the most active compound. newline