Synthesis and antimicrobial activity of s-substituted derivatives of 1,2,4-triazol-3-thiol

The aim of the work. 1,2,4-triazole derivatives possess a wide range pharmacological activity, so they are used for development drugs and active pharmaceutical ingredients. Due to reactivity 1,2,4-triazoles there many options their further structural modification on different reaction centers. Therefore, work was obtain new S-substituted 1,2,4-triazole-3-thiols, study physicochemical parameters substances synthesized, evaluate antimicrobial activity S-derivatives 4-R1-5-((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazole-3-thiol series, some regularities “structure – biological activity” relationship synthesized compounds as well.
 Materials methods. subject containing 2-oxopropan-1-yl 2-aryl-2-oxoethan-1-yl substituents. studied by double serial dilutions test cultures Staphylococcus aureus (ATCC 25923), Escherichia coli 25922), Pseudomonas aeruginosa 27853), Candida albicans 885-653).
 results screening showed that at concentration 125 g/mL, all (MIC in 31.25 - 62.5 ?g/mL, MBCK 62.5–125 ?g/mL) against strains coli, aureus, aeruginosa, albicans. Variation substituents sulfur atom did not lead significant change antifungal activities among 4-R1-5-((3-(pyridin-4-yl)-1H-1,2,4-triazole-5-yl) thio)methyl)-4H-1,2,4-triazole-3-thiols.
 Conclusions. Biological data indicate prospects search abovementioned 1,2,4-triazoles. most were 1-((4-ethyl-5-((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazol-3-yl)thio)propan-2-one 1-(4-methoxyphenyl)-2-(4-ethyl-5-(((3-(pyridin-4-yl)-1H)-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazol-3-yl)thio)ethanone, which pronounced strain MBcK