АНТИБАКТЕРИАЛЬНАЯ АКТИВНОСТЬ 3-АРИЛИМИНОМЕТИЛХРОМОНОВ

Abstract

In conditions of multiple drug resistance of microorganisms to recently used drugs, the search for new chemotherapeutic agents with a pronounced bactericidal or bacteriostatic effect with low toxicity and teratogenicity remains relevant. Chromone derivatives with a wide spectrum of pharmacological activity (membrane-stabilizing, antiviral, antibacterial, anti-inflammatory, cardioprotective, antioxidant) are promising compounds for the search for new generation chemotherapeutic drugs. As a result of the study, it was found that gram-positive bacteria Staphylococcus aureus shows the highest sensitivity to the studied compounds when growing on a liquid nutrient medium. The studied compounds are also active against pathogenic strains of Bacillus cereus, Escherichia coli. The minimum inhibitory concentration (IPC) of the most active substances in relation to St. strains aureus is 10 μg/ml for 7-acetoxy-3-(p-bromophenyl)iminomethylchromone, and for 3-(p-bromophenyl)-iminomethylchromone and 7-acetoxy-3-(p-sulfamidophenyl)iminomethylchromone – 20 μg/ml. For 7-acetoxy-3- (p-bromophenyl)iminomethylchromone and 3-(p-bromophenyl)iminomethylchromone, a high antibacterial activity was revealed with respect to the spore-forming bacteria Bacillus subtilis – MPC – 20 μg / ml. The synthesized compounds exhibit a low bacteriostatic activity with respect to the Pseudomonas aeruginosa strain. Experimental studies have shown that the nature and position of substituents in the structure of 3–aryliminomethylchromones affects their antibacterial activity against strains of gram-positive bacteria Staphulococcus aureus and Bacillus subtilis, a strain of gram-negative bacteria: Escherichia coli. The presence in the series of synthesized 3–aryliminomethylchromones of compounds with high bacteriostatic activity at the level of an antibacterial drug from the group of sulfonamides – norsulfazole was established.