Design, synthesis and antifungal evaluation of novel benzimidazole tertiary amine type of fluconazole analogues

Abstract

A novel series of compounds containing tertiary amine moiety, substituted benzimidazole and triazole ring, initial design by molecular docking study of this scaffold at the active site of the fungal enzymes lanosterol 14α-demethylase (homology modeled of C. albicans) was synthesized by microwave irradiation and characterized by Proton Nuclear Magnetic Resonance (1H NMR), Infra Red (IR), and Mass Spectroscopy (MS), and by elemental analysis. The screening of compound for in vitro (turbidimetric method) and in vivo (kidney burden test) antifungal activity against C. albicans revealed activity in many of the compounds as comparable to that of fluconazole. Keywords: Benzimidazole, Triazole, Antifungal, Lanosterol 14-α-demethylase, Microwave irradiation, Docking