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Synthesis, evaluation and binding mode analysis of some novel triazole derivatives as antimicrobials


Subhasis Banerjee , Swastika Ganguly , Kalyan Kumar Sen , Kiattawee Choowongkomon , Supaporn Seetaha

Abstract

A series of twenty seven novel N-(substituted phenyl)-2-(1H-1,2,4-triazol-1- yl)acetamides 3(a-i), 2-[(4-amino-5-phenyl-4H-1,2,4-triazol-3-yl) thio]-N- (substituted phenyl) acetamides 5(a-i) and 2-[(4-amino-5- pyridin-3-yl-4H-1,2,4- triazol-3-yl)thio]-N-(substituted phenyl) acetamides 7(a-i) were synthesized by reacting 1H-1,2,4-triazole (2), 4-amino-5-pyridin-3-yl-4H-1,2,4-triazole-3-thiol (4) and 4-amino-5-phenyl-4H-1,2,4-triazole-3-thiol (5) with the respective 2-chloro-N- (substituted phenyl) acetamides 1(a-i) in acetonitrile and triethylamine. Structure elucidation of all the synthesized compounds was made on the basis of the data obtained out of various spectral studies. All the synthesized compounds were evaluated for HIV-1 reverse transcriptase (RT) inhibitory activity, antibacterial and antifungal activities. Compound 7i was the most promising among all with 52% HIV inhibition. Most of the compounds showed comparable antifungal activity against Candida spp with respect to the standard antifungal agent fluconazole, whereas they exhibited weak inhibitory property against pathogenic bacteria taken for the study. Docking studies with reverse transcriptase enzyme of (PDB entry code 1RT2) was also performed for the highest active compound 7i in order to investigate the binding pattern of the same.



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