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二苯基二硒醚及其合成类似物的体外抗真菌评价及构效关系。

In vitro antifungal evaluation and structure-activity relationship of diphenyl diselenide and synthetic analogues.

机构信息

Departamento de Química, Centro de Ciências Naturais e Exatas, Universidade Federal de Santa Maria, RS, Brazil.

出版信息

Mycoses. 2011 Sep;54(5):e572-6. doi: 10.1111/j.1439-0507.2010.01994.x. Epub 2011 May 25.

DOI:10.1111/j.1439-0507.2010.01994.x
PMID:21615531
Abstract

We report on in vitro antifungal activity and the structure-activity relationship of diphenyl diselenide [(PhSe)(2) ] and its synthetic analogues, (p-Cl-C(6) H(4) Se)(2), (m-CF(3)-C(6) H(4)Se)(2) and (p-CH(3)O-C(6) H(4)Se)(2), against 116 strains of pathogenic fungi. (PhSe)(2) showed the highest inhibitory activity against Candida albicans (minimum inhibitory concentration of 4-32 μg ml(-1) ), Candida dubliniensis (2-16 μg ml(-1)), Aspergillus spp. (0.5-64 μg ml(-1)) and Fusarium spp. (2-16 μg ml(-1)). Its minimum fungicidal concentration (MFC) varied among C. albicans (4-64 μg ml(-1)), C. dubliniensis (2-32 μg ml(-1) ) and Fusarium spp. (4-64 μg ml(-1)). Antifungal activity was decreased by the introduction of functional groups to the (PhSe)(2) molecule: (PhSe)(2) >(p-CH(3)O-C(6)H(4) Se)(2) >(m-CF(3)-C(6)H(4)Se)(2) >(p-Cl-C(6) H(4)Se)(2).

摘要

我们报告了二苯基二硒醚[(PhSe) 2]及其合成类似物((p-Cl-C 6 H 4 Se) 2、(m-CF 3 -C 6 H 4 Se) 2和(p-CH 3 O-C 6 H 4 Se) 2)的体外抗真菌活性和构效关系,针对 116 株致病真菌。(PhSe) 2对白色念珠菌(最低抑菌浓度为 4-32 μg ml(-1))、都柏林念珠菌(2-16 μg ml(-1))、曲霉菌属(0.5-64 μg ml(-1))和镰刀菌属(2-16 μg ml(-1))表现出最高的抑制活性。其最小杀菌浓度(MFC)在白色念珠菌(4-64 μg ml(-1))、都柏林念珠菌(2-32 μg ml(-1))和镰刀菌属(4-64 μg ml(-1))中有所不同。在(PhSe) 2分子中引入官能团会降低抗真菌活性:(PhSe) 2>(p-CH 3 O-C 6 H 4 Se) 2>(m-CF 3 -C 6 H 4 Se) 2>(p-Cl-C 6 H 4 Se) 2。

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