title: Synthesis and anticandidal activity of new triazolothiadiazine derivatives.
abstract: New triazolothiadiazine derivatives were synthesized via the ring closure reaction of 4-amino-5-substituted-2,4-dihydro-3H-1,2,4-triazol-3-thiones with phenacyl bromides. The compounds were tested in vitro against various Candida species and compared with ketoconazole. Among these compounds, the compound bearing cyclohexyl moiety and p-chlorophenyl substituent on triazolothiadiazine ring (2i) was found to be the most potent derivative against Candida albicans (ATCC 90028). It is clear that there is a positive correlation between anticandidal activity and two functional moieties, namely cycloaliphatic group and p-chlorophenyl substituent on triazolothiadiazine ring. The compounds were also investigated for their cytotoxic effects using MTT assay. Compound 2a exhibited the highest cytotoxic activity, whereas compound 2f possessed the lowest cytotoxic activity against NIH/3T3 cells.
authors.affiliation: Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 26470 Eskişehir, Turkey.
authors.forename: Mehlika Dilek
authors.initials: MD
authors.lastname: Altıntop
authors.forename: Zafer Asım
authors.initials: ZA
authors.lastname: Kaplancıklı
authors.forename: Gülhan
authors.initials: G
authors.lastname: Turan-Zitouni
authors.forename: Ahmet
authors.initials: A
authors.lastname: Özdemir
authors.forename: Gökalp
authors.initials: G
authors.lastname: İşcan
authors.forename: Gülşen
authors.initials: G
authors.lastname: Akalın
authors.forename: Şafak  Ulusoylar
authors.initials: Ş
authors.lastname: Yıldırım
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002175:Candida / Q000187:drug effects*; D060326:Chemistry Techniques, Synthetic; D055808:Drug Discovery; D051379:Mice; D008826:Microbial Sensitivity Tests; D041681:NIH 3T3 Cells; D013829:Thiadiazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000935:Antifungal Agents; D013829:Thiadiazines