Synthesis and mycological activity of the compounds obtained in the reaction of N(3)-substituted amidrazones with sulphinyl-bis-2,4-dihydroxybenzenethioyl.
2-Phenyl-5-(2,4-dihydroxybenzene)-1,3,4-thiadiazole (4), 2-(2-pyridyl)-2,4-dihydroxybenzene-1,3,4-thiadiazole (5), N(1)-2,4-dihydroxybenzenecarbothio-N(3)-phenyl-benzamidrazone (6) and N(1)-2,4-dihydroxybenzenecarbothio-N(3)-phenyl-2-picoline-amidrazone (7) were prepared and tested for their antimycotic activity. The chemical structures were confirmed by IR, 1H-NMR, EI-MS and elemental analysis. The minimal inhibitory concentration (MIC) values against dermatophytes, yeasts and moulds were determined for the estimation of potential activity in vitro. The strongest fungistatic activity for compound 5 in relation to dermatophytes was found with MIC 0.48-0.99 microg mL(-1).
Department of Organic Chemistry, Faculty of Pharmacy, Medical University, Lublin, Poland. jmaty@agros.ar.lublin.pl
B
B
Modzelewska-Banachiewicz
J
J
Matysiak
A
A
Niewiadomy
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D003883:Arthrodermataceae / Q000187:drug effects*; D001549:Benzamides / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D010847:Picolines / Q000494:pharmacology*; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology*; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology*; D015003:Yeasts / Q000187:drug effects*
C425342:2-(2-pyridyl)-2,4-dihydroxybenzene-1,3,4-thiadiazole; C425341:2-phenyl-5-(2,4-dihydroxybenzene)-1,3,4-thiadiazole; D000935:Antifungal Agents; D001549:Benzamides; C425343:N1-2,4-dihydroxybenzenecarbiothio-N3-phenyl-2-picolineamidrazone; D010847:Picolines; D011725:Pyridines; D013830:Thiadiazoles