EVALUATION OF THE ANTIMICROBIAL ACTIVITY OF 5-HYDROXY(SULFANYL) [1,2,3]TRIAZOLO[4,5-e][1,4]DIAZEPINES

Abstract

A short literary summary of the article focuses on the grave danger of infectious diseases, which lead to high morbidity and mortality. It is noted that the emergence of resistance of bacterial pathogens to old and new antibiotics has led to the need for new types of antibacterial agents in the last decade. That is why 5-hydroxy[1,2,3]triazolo[4,5-e][1,4]diazepines were used as new objects for investigation of antimicrobial action, were previously synthesized by the authors by intramolecular cyclocondensation of 5-amino-N-(2,2-dimethoxyethyl)-1H-1,2,3-triazolo-4-carboxamide in muric acid and their 5-sulfanyl derivatives obtained from 5-hydroxy derivatives action by S-nucleophiles. The results of bioscreening of 5-hydroxy[1,2,3]triazolo[4,5-e] [1,4]diazepines derivatives show that they exhibit moderate antimicrobial activity (minimum inhibitory concentration (MIC) was 31.25-125 mcg/ml) and moderate antifungal activity (MIC was 31.25-62.5 mcg/ml). At the same time, the activity in relation to test strains of bacteria Staphylococcus aureus and Bacillus cereus for the tested series of spores is not selective: МІК = 125 μg/ml (Staphylococcus aureu) and МІК = 62.5 μg/ml (Bacillus cereus). 5-Sulfanilsubstituted [1,2,3]triazolo[4,5-e] [1,4]diazepines exhibit bacteriostatic activity in the concentration range of 31.25-125 μg/ml and fungistatic effect at MІK = 31.25 μg/ml. Regarding their activity to test strains of bacteria Bacillus cereus and fungi Candida albicans and Aspergillus niger K9, it is not selective, the minimum inhibitory concentration is 31.25 μg/ml for all three types of these microbes. In relation to Staphylococcus aureus and Escherichia coli 25922 test strains, the spores with the thioalkylcarboxylic acid fragment deserve special attention as they exhibit an order of magnitude higher activity than their analogues of the studied series.