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抗菌和抗真菌剂的研究,X. 1-(对甲基-α-[4-(1H-吡咯-1-基)苯基]苄基)唑类及一些相关产物的合成与抗真菌活性

Researches on antibacterial and antifungal agents, X. Synthesis and antifungal activities of 1-(p-methyl-alpha-[4-(1H-pyrrol-1-yl)phenyl]benzyl)azoles and some related products.

作者信息

Massa S, Stefancich G, Corelli F, Silvestri R, Mai A, Artico M, Panico S, Simonetti N

出版信息

Arch Pharm (Weinheim). 1989 Jun;322(6):369-73. doi: 10.1002/ardp.19893220609.

DOI:10.1002/ardp.19893220609
PMID:2774871
Abstract

The synthesis and antifungal activities against Candida albicans and Candida spp. of some pyrrole analogues of bifonazole are reported. 1-(p-Methyl-alpha-[4-(1H-pyrrol-1-yl)phenyl]benzyl)imidazole was found to be equipotent or sometimes superior to bifonazole and ketoconazole, and lightly inferior to miconazole. Substitution of the imidazole moiety with other azoles retained some activities. No activity was shown when the azole aromatic rings were replaced by the heteroalicyclic ones.

摘要

报道了联苯苄唑的一些吡咯类似物的合成及其对白色念珠菌和念珠菌属的抗真菌活性。发现1-(对甲基-α-[4-(1H-吡咯-1-基)苯基]苄基)咪唑与联苯苄唑和酮康唑效力相当,有时甚至优于它们,略逊于咪康唑。用其他唑类取代咪唑部分仍保留一些活性。当唑类芳香环被杂脂环取代时则无活性。

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