Synthesis and anticandidal activity of new triazolothiadiazine derivatives

被引：30

作者：

Altintop, Mehlika Dilek ^{[1
]}

Kaplancikli, Zafer Asim ^{[1
]}

Turan-Zitouni, Gulhan ^{[1
]}

Ozdemir, Ahmet ^{[1
]}

Iscan, Gokalp ^{[2
]}

Akalin, Gulsen ^{[3
]}

Yildirim, Safak Ulusoylar ^{[4
]}

机构：

[1] Anadolu Univ, Fac Pharm, Dept Pharmaceut Chem, TR-26470 Eskisehir, Turkey

[2] Anadolu Univ, Fac Pharm, Dept Pharmacognosy, TR-26470 Eskisehir, Turkey

[3] Anadolu Univ, Fac Pharm, Dept Biochem, TR-26470 Eskisehir, Turkey

[4] Anadolu Univ, Fac Pharm, Dept Pharmacol, TR-26470 Eskisehir, Turkey

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 11期

关键词：

Triazole; Triazolothiadiazine; Anticandidal activity; Cytotoxicity; INVASIVE CANDIDIASIS; ANTIFUNGAL; EPIDEMIOLOGY; TRIAZOLE;

D O I：

10.1016/j.ejmech.2011.09.020

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 (21) 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. (C) 2011 Elsevier Masson SAS. All rights reserved.

引用

页码：5562 / 5566

页数：5

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