Synthesis, antimicrobial and antifungal activity of ylidenhydrazides of 2-((4-R-5-R1-4H-1,2,4-TRIAZOL-3-YL)THIO) acetaldehydes

Abstract

Objective: The aim of this work is the synthesis and studying of antimicrobial and antifungal properties of the ylidenhydrazides of 2-((4-R-5-R1-4H-1,2,4-triazol-3-yl)thio)acetaldehydes with the establishment of structure-activity relationships of the synthesized compounds. Material and Method: Determination of antimicrobial and antifungal activity was performed by discdiffusion method (DDM) on series of gram positive and gram negative bacteria such as Corynebacterium pseudodiphtheriticum, Pseudomonas aeruginosa, Enterococcus faecalis, Proteus vulgaris, Escherichia coli, Salmonella spp., Staphylococcus saprophyticus, Staphylococcus aureus, Streptococcus pyogenes, Candida. Result and Discussion: A new series of ylidenhydrazides of 2-((4-R-5-R1-4H-1,2,4-triazol-3- yl)thio)acetaldehydes were synthesized and their structures were confirmed by modern methods of instrumental analysis: IR and 1H-spectroscopy, elemental analysis and GS\MS method. For 13 compounds, the antimicrobial and antifungal activities were studied on 10 strains of microorganisms in 3 different concentrations (0.1; 0.2; 0.5%). According to the results of the study, some regularities of the structureactivity relationship have been established. The obtained results can serve as a basis for the targeted search compounds with pronounced antibacterial action. An increasing the concentration of tested compounds predictably lead to increase on antimicrobial activity in almost all cases. The most active compound in our study is N'-(2-((5-methyl-4H-1,2,4-triazol-3-yl)thio)ethylidene)-4-nitrobenzohydrazide 3i (ZOI for Sta.s. and Sp in 0.5% concentration is 25 and 26 mm, respectively).