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卤代富马酸酯的抗真菌特性。

Antifungal properties of halofumarate esters.

作者信息

Gershon H, Shanks L

出版信息

J Pharm Sci. 1978 Apr;67(4):578-80. doi: 10.1002/jps.2600670443.

DOI:10.1002/jps.2600670443
PMID:641780
Abstract

Alkyl esters (C1--C4) of the four halofumaric acids were tested for antifungal activity against Candida albicans, Aspergillus niger, Mucor mucedo, and Trichophyton mentagrophytes at pH 5.6 and 7.0 in the absence and presence of 10% beef serum in Sabouraud dextrose agar. The most toxic compound to each organism was: C. albicans, ethyl iodofumarate (0.054 mmole/liter); A. niger, methyl bromofumarate (0.090 mmole/liter); M. mucedo, methyl fluorofumarate (0.037 mmole/liter); and T. mentagrophytes, ethyl iodofumarate (0.020 mmole/liter). The order of overall activity of the six most toxic compounds was: ethyl iodofumarate greater than ethyl chlorofumarate greater than methyl iodofumarate = methyl bromofumarate greater than methyl chlorofumarate greater than bromofumarate.

摘要

在pH值为5.6和7.0的条件下,于不含和含有10%牛血清的沙氏葡萄糖琼脂中,测试了四种卤代富马酸的烷基酯(C1 - C4)对白色念珠菌、黑曲霉、毛霉和须癣毛癣菌的抗真菌活性。对每种生物体毒性最大的化合物分别是:白色念珠菌,碘代富马酸乙酯(0.054毫摩尔/升);黑曲霉,溴代富马酸甲酯(0.090毫摩尔/升);毛霉,氟代富马酸甲酯(0.037毫摩尔/升);须癣毛癣菌,碘代富马酸乙酯(0.020毫摩尔/升)。六种毒性最大的化合物的总体活性顺序为:碘代富马酸乙酯>氯代富马酸乙酯>碘代富马酸甲酯 = 溴代富马酸甲酯>氯代富马酸甲酯>溴代富马酸。

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