SYNTHESIS, PHYSICOCHEMICAL PROPERTIES, ANTIMICROBIAL AND FREE-RADICAL SCAVENGING ACTIVITY OF SUBSTITUTED BENZO[4,5]IMIDAZO[1,2-C]QUINAZOLINE-6(5H)-ONES (-THIONES)

Abstract

This study describes the elaboration of synthetic procedures for 6-S-subtituted and 5-N-substituted benzo[4,5]imidazo[1,2-c]quinazolines, as well as their antiradical and antimicrobial activity screening results. It has been showed that target substances can be prepared by alkylation of initial potassium benzo[4,5]imidazo[1,2-с]quinazolin-6-thiolate and benzo[4,5]imidazo[1,2-c]quinazolin-6(5H)-one with substituted 2-chloracetamides in appropriate conditions. The features of synthesized compounds’ NMR spectra have been investigated and discussed. It has been found out that 2-(6-oxobenzo[4,5]imidazo[1,2-c]quinazoline-5(6H)-yl)acetamides  do not reveal antiradical activity, while most of 6-S-substituted benzo[4,5]imidazo[1,2-с]quinazolines are active free radical scavenging agents. The conducted study of synthesized compound`s antibacterial and antifungal activity revealed their low or moderate activity against E. coli, S. aureus and P. aeruginosa strains. An opportunistic pathogenic yeast C. albicans has been identified as the most susceptible to synthesized compounds strain. The reliable correlation between the nature of substituent at acetamide Nitrogen and antimicrobial activity has not been found. It has been substantiated that studied classes of compound are promising objects for the search of chemotherapeutic agents.