SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL EVALUATION OF NOVEL BIS-HETERO CYCLIC DERIVATIVES

Abstract

The present research outlines a series of bis-hetero cyclic derivatives (a1-6) synthesized from methyl-1-(2, 5-dioxopyrrolidin-1-yl) -6- methyl -2- oxo -4- phenyl -1, 2, 3, 4- tetrahydro pyrimidine -5- carboxylate treated with different aromatic aldehydes under acidic environment. The synthesized titled derivatives were confirmed by determination of physicochemical properties, by different spectral data and they were evaluated for in vitro antibacterial activity against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa and antifungal activity against Aspergillus niger and Candida albicans organisms at 25, 50, 100 µg mL-1 concentrations using streptomycin and fluconazole as reference standard drug respectively, through cup plate method. The in vitro antimicrobial assay results indicated that the derivatives a1, a2 and a3 showed significant antimicrobial activity, whereas the remaining derivatives showed moderate antimicrobial activities compared to the standard drugs. Further extension of this research to the cellular level is required to describe the mechanism of action, efficacy, and structural activity of these derivatives for antimicrobial activity.