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四种抗真菌苯并噻唑的抗念珠菌活性。

Anti-Candida activity of four antifungal benzothiazoles.

作者信息

Bujdáková H, Kuchta T, Sidóová E, Gvozdjaková A

机构信息

Department of Microbiology and Virology, Faculty of Science, Comenius University, Bratislava, Slovak Republic.

出版信息

FEMS Microbiol Lett. 1993 Sep 15;112(3):329-33. doi: 10.1111/j.1574-6968.1993.tb06471.x.

DOI:10.1111/j.1574-6968.1993.tb06471.x
PMID:8224799
Abstract

Anti-Candida activity of 6-amino-2-n-pentylthiobenzothiazole (I), benzylester of (6-amino-2-benzothiazolylthio)acetic acid (II) and of 3-butylthio-(1,2,4-triazolo)-2,3-benzothiazole (III) was followed and compared to that of 2-mercaptobenzothiazole (IV). I and II exhibited good activity against the C. albicans yeast form, similar to IV. They were inhibitorily active against other Candida strains, IC50 values being of the order of 10(-5) M, which means better activity than IV. Compound I also exhibited inhibitory activity on germ-tube formation and mycelial growth in the C. albicans strains, while II, III and IV were not active in these tests. III was the least active form of the compounds tested, IC50 values being of the order of 10(-4) M. All the compounds tested were highly active on a nystatin-resistant C. albicans mutant, with IC50s of the order of 10(-6) M-10(-5) M.

摘要

对6-氨基-2-正戊基硫代苯并噻唑(I)、(6-氨基-2-苯并噻唑基硫代)乙酸苄酯(II)和3-丁基硫代-(1,2,4-三唑并)-2,3-苯并噻唑(III)的抗念珠菌活性进行了跟踪,并与2-巯基苯并噻唑(IV)的活性进行了比较。I和II对白色念珠菌酵母形态表现出良好的活性,与IV相似。它们对其他念珠菌菌株具有抑制活性,IC50值约为10^(-5) M,这意味着其活性优于IV。化合物I对白色念珠菌菌株的芽管形成和菌丝生长也表现出抑制活性,而II、III和IV在这些测试中无活性。III是所测试化合物中活性最低的形式,IC50值约为10^(-4) M。所有测试化合物对耐制霉菌素的白色念珠菌突变体均具有高活性,IC50值为10^(-6) M - 10^(-5) M。

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