Hybrids Of Fluconazole: Synthesis and Antimicrobial Activity

Abstract

Based on the structure of the active site of cytochrome P450 14α-demethylase (CYP51) a series of 1-(1-(substituted phenyl)-2-(1H-1,2,4-triazol-1-yl)ethylidene)-2-(1-(substututed phenyl)-2-(1H-1,2,4-triazol-1-yl)ethylidene)hydrazine of fluconazole analogues were synthesized starting from phenacyl bromide (0.01 mol) and 1,2,4 triazole. All compounds were characterized by advanced tools like IR, ¹H-NMR, ¹³C-NMR, mass spectroscopy and elemental analysis. All the synthesized compounds were tested qualitative (Zone of inhibition) and quantitative (MIC) antimicrobial activities against four pathogenic bacteria B. subtilis, S. aureus, E. coli and P. aeruginosa and two pathogenic fungi C. albicans and A. niger. Most of the synthesized screened compounds showed potent antimicrobial activity against gram positive and gram negative bacteria as well as fungi species.