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抗真菌剂,II:含不饱和链的芳基-1H-吡咯-2-基-1H-咪唑-1-基甲烷衍生物的合成及抗真菌活性

Antifungal agents, II: Synthesis and antifungal activities of aryl-1H-pyrrol-2-yl-1H-imidazol-1-yl-methane derivatives with unsaturated chains.

作者信息

Massa S, Ragno R, Porretta G C, Mai A, Retico A, Artico M, Simonetti N

机构信息

Dipartimento di Studi Farmaceutici, Università La Sapienza, Roma, Italy.

出版信息

Arch Pharm (Weinheim). 1993 Sep;326(9):539-46. doi: 10.1002/ardp.19933260909.

Abstract

The synthesis and antifungal activities of aryl-1H-pyrrol-2-yl-1H-imidazol-1-yl-methanes having allyl, crotyl, and acrylate chains linked to the N-pyrrole atom and substituted at phenyl ring by Cl, F, CH3, and NO2 groups are reported. In vitro tests against Candida albicans and Candida spp. showed 2,4-dichlorophenyl-1-allyl-1H-pyrrol-2-yl-1H-imidazol-1-yl-methane to be the most potent derivative with activities comparable to those of ketoconazole and slightly inferior to those of bifonazole and miconazole. Some structure-activity relationships are discussed.

摘要

报道了在N-吡咯原子上连接有烯丙基、巴豆基和丙烯酸酯链且在苯环上被氯、氟、甲基和硝基取代的芳基-1H-吡咯-2-基-1H-咪唑-1-基甲烷的合成及其抗真菌活性。针对白色念珠菌和念珠菌属的体外试验表明,2,4-二氯苯基-1-烯丙基-1H-吡咯-2-基-1H-咪唑-1-基甲烷是最有效的衍生物,其活性与酮康唑相当,略逊于联苯苄唑和咪康唑。讨论了一些构效关系。

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