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- Title
SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME 3,5-DISUBSTITUTED-TETRAHYDRO-2H-1,3,5-THIADIAZINE- 2-THIONE DERIVATIVES.
- Authors
Sağlam, Evren; Saraç, Selma; Kiliç, Ekrem; Özalp, Meral; Ertan, Mevlüt
- Abstract
A series of new 3,5-disubstituted-tetrahydro-2H-1,3,5-thiadiazine-2-thione (THTT) derivatives (4a-g) were prepared using a convenient and general one-pot procedure and evaluated for their in vitro antibacterial and antifungal activities by using the microdilution method in comparison with ampicillin and fluconazole. 3-Phenyl-5-(1-phenylethyl)-tetrahydro-2H-1,3,5-thiadiazine-2-thione (4a) and 3- phenyl-5-hydroxy-tetrahydro-2H-1,3,5-thiadiazine-2-thione (4g) were found to be active against Staphylococcus aureus and Enterococcus faecalis with MIC values of 4 and 16 μg/mL, respectively. The antifungal activity of 3-phenyl-5-(1-phenylethyl)-tetrahydro-2H-1,3,5-thiadiazine-2-thione (4a) against Candida krusei and C. parapsilosis appeared greater than that of fluconazole (MIC: 64 μg/mL and 8 μg/mL) with MIC of 8 and 4 μg/mL, respectively. 3-Phenyl-5-(1-phenylethyl)-tetrahydro-2H-1,3,5- thiadiazine-2-thione (4a) also exhibited antifungal activity against C. albicans with a MIC of 4 μg/mL. The antifungal activity of 3-(1-phenylethyl-5-[a-(isobutyl)carboxymethyl]-tetrahydro-2H-1,3,5- thiadiazine-2-thione (4b) and 3-benzyl-5-carboxyethyl-tetrahydro-2H-1,3,5-thiadiazine-2-thione (4c) against C. krusei were found to be similar to that of fluconazole (MIC: 64 μg/mL).
- Subjects
HYDROXYLAMINE; PRODRUGS; ANTIBODY-directed enzyme prodrug therapy; ANTIBACTERIAL agents; ANTIFUNGAL agents
- Publication
Turkish Journal of Pharmaceutical Sciences, 2011, Vol 8, Issue 2, p159
- ISSN
1304-530X
- Publication type
Article