The study of antimicrobial activity of 2-((4-R-3-(morpholinomethylene)-4H-1,2,4-triazole-5-yl)thio)acetic acid salts

The purpose of the work was to study the antimicrobial activity of 2-((4-R-3-(morfolinomethylene)-4 H -1,2,4-triazole-5-yl)thio) acetic acid salts by "hanging drop" and “serial dilution” methods in broth (limiting concentration option) and establish some patterns of "structure – action" depending. Materials and methods. The objects of research were 9 new compounds of 2-((4-R-3-(morfolinomethylene)-4 H -1,2,4-triazole-5-yl)thio) acetic acid salts. These compounds are the crystal substances which are odorless, soluble in water and organic solvents. To achieve a more objective picture of the research we applied two methods: "hanging drop" and “serial dilution” in broth (limiting concentration option). To study the effectiveness of substances we used the test cultures of E. coli , Salmonella typhymurium , Staphylococcus epidermidis, P. aeruginosa . Results and discussion. In the study we have found that 2-((4-R-3-(morfolinomethylene)-4 H -1,2,4-triazole-5-yl)thio) acetic acid salts can differently inhibit the growth of test cultures. The results show that the data obtained by two methods correlated with each other. Thus, the 2-((4-R-3-(morfolinomethylene)-4 H -1,2,4-triazole-5-yl)thio) acetic acid salts are active against most strains of E. Coli . and Salmonella typhymurium . Analyzing the impact of 2-((4-R-3-(morfolinomethylene)-4 H -1,2,4-triazole-5-yl)thio) acetic acid salts we have noted that the replacement of the phenyl radical (PKR-135, 139) on the free amino group at N4 nitrogen of 1,2,4- triazole cycle (PKR-173, 177) leads to the disappearance of antimicrobial activity against the studied strains. It was established that the transition from morfolin cation (PKR-133) to the piperydyn cation (PKR-134) in the molecules of 2-((4-phenyl-3-(morfolinometylen)-4 H -1,2,4-triazole-5-yl) thio) acetic acid is accompanied by a significant increase in antimicrobial effect. It was interesting that among all the cations in the molecules of 2-((4-amino-3-(morfolinometylen)-4H-1,2,4-triazole-5-yl) thio) acetic acid salt (PKR-173, 174, 177, 234) only the presence of sodium cation (PKR-174) leads to a pronounced antimicrobial effect against studied strains. Conclusions. The study had found that the most effective in relation to the main groups of pathogenic bacteria are substances PKR-134, 135, 136, 139 and 174. Certain regularities based on "structure-action" have been established, this information can be integrated into future targeted search of substances with antimicrobial properties.