Design, Synthesis, Characterisation and Antifungal Activity of Novel Pyrimidone Derivatives

Abstract

Pyrimidones and oxadiazoles possess a wide range of biological activities such as antibacterial, antifungal, analgesic, anti-inflammatory and anticancer activities. The prevalence of fungal infections has progressively increased in recent years and hence it is necessary to continue the search for new, less toxic and more efficacious antifungal agents. As vast number of reports are available pertaining to the antifungal activities of pyrimidones and oxadiazoles, combination of these two moieties may result in additive effect towards antifungal activity. The aim of the present study was to design and synthesize some hybrid molecules containing both pyrimidone and oxadiazole moieties in order to evaluate their antifungal activity. Virtual screening was carried out through molecular docking studies against potential antifungal target glycolipid 2α-mannosyl transferase. Ten novel pyrimidone derivatives were synthesized and characterized using UV, IR, HNMR and Mass spectroscopy analysis. The antifungal activity of newly synthesized pyrimidone derivatives was evaluated by Zone inhibition method against two antifungal strains Aspergillus niger and Candida albicans.