SEARCH FOR EFFECTIVE DRUGS AGAINST PATHOGENIC FLORA IN THE SERIES OF O-para-TOLUOYL-β-(MORPHOLIN-1-YL)PROPIOMIDOXIME AND 5-ARYL-3-β-(PIPERIDINE-1-YL)ETHYL-1,2,4-OXADIAZOLES DERIVATIVES

Abstract

Abstract. Introduction. In the context of the growing resistance of pathogenic microorganisms to traditional antibiotics, as well as the increase in the number of fungal infections, it is important to find new effective agents to combat these threats. Objectives and tasks. The work is devoted to the study of antimicrobial and antifungal activity of β-aminopropioamidoxime derivatives. Methods. In the chemical part of the work, two groups of compounds were obtained: O-para-toluoyl-β-(morpholin-1-yl)propioamidoxime base, hydrochloride, oxalate, citrate and 5-aryl-3-β-(piperidin-1-yl)ethyl-1,2,4-oxadiazoles (aryl: para-MeC₆H₄, para-BrC₆H₄, meta-ClC₆H₄), described earlier. Using in vitro microbiological screening, β-aminopropioamidoxime derivatives were tested for antimicrobial (on gram-positive bacteria Staphylococcus aureus, Bacillus subtilis and on gram-negative bacteria Escherichia coli, Pseudomonas aeruginosa), as well as for antifungal activity against the yeast strain Candida albicans and mold fungi Penicillium citrinum, Aspergillus niger, Torulla spp. Results. The β-aminopropioamidoxime derivatives studied by the agar diffusion (well) method and the serial dilution method have pronounced antimicrobial activity. Using serial dilution method it was determined that O-para-toluoyl-β-(morpholin-1-yl)propioamidoxime oxalate, with lower toxicity than the reference drugs gentamicin and nystatin (LD₅₀, mg/kg), exhibits equal antimicrobial activity against Staphylococcus aureus and antifungal activity against Candida albicans. Conclusion. Antimicrobial and antifungal properties were found in β-aminopropioamidoxime derivatives. O-para-toluoyl-β-(morpholin-1-yl)propioamidoxime oxalate was determined as a promising compound for the use in medicine and agriculture.