1. Search for Biologically Active Substances with Antimicrobial and Antifungal Action in the series of 2.5-disubstituted 1, 3, 4-tiadiazoles
- Author
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Igor V. Sych, Iryna V. Drapak, Marharyta M. Suleiman, Maryna V. Rakhimova, Natalya P. Kobzar, Irina A. Sych, and Lina O. Perekhoda
- Subjects
Antifungal ,biology ,medicine.drug_class ,Nuclear magnetic resonance spectroscopy ,biology.organism_classification ,Antimicrobial ,Combinatorial chemistry ,Acylation ,chemistry.chemical_compound ,chemistry ,Sulfanyl ,medicine ,Pharmacology (medical) ,Candida albicans ,Benzamide ,Pharmacology, Toxicology and Pharmaceutics (miscellaneous) ,Bacteria - Abstract
A range of derivatives of sulfonyl-substituted nitrogen-containing heterocyclic systems has been extended by synthesis of 2N (R)-5R1-1,3,4-thiadiazol-2-yl-arylsulfonamides and N-(diethylsulfamoyl)-N-(5-ethyl-1,3,4-thiadiazol-2-yl)benzamides. It was established that acylation of 5-ethylsulfanyl-1,3,4-thiadiazole-2-amine by heteryl-substituted acid chlorides allowed for obtaining not reported in the literature heterocyclic compounds, which structure contained two cycles of 1,3,4-thiadiazole. The structure and purity of the obtained compounds was confirmed by 1? NMR-spectroscopy, elemental analysis, and thin-layer chromatography. Pharmacological studies on antimicrobial and antifungal activity have shown that all the compounds tested have sensitivity to both Gram-positive, and Gram-negative bacteria. In addition, the obtained substances have exhibited antifungal activity against Candida albicans. The studies have identified compound 4-butoxy-N-{5-[({[5- (ethylsulfanyl)-1,3,4-thiadiazol-2-yl] carbomoyl} methyl) sulfanyl] -1,3,4-thiadiazol-2-yl} benzamide with high antimicrobial activity further studies of which are promising.
- Published
- 2019