Novel antifungal 2-aryl-1-(1H-1,2,4-triazol-1-yl)butan-2-ol derivatives with high activity against Aspergillus fumigatus.

被引：88

作者：

Dickinson, RP

Bell, AS

Hitchcock, CA

Narayanaswami, S

Ray, SJ

Richardson, K

Troke, PF

机构：

[1] Pfizer Central Research, Sandwich

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 16期

关键词：

D O I：

10.1016/0960-894X(96)00363-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Replacement of one triazole ring of fluconazole with 4-pyridinyl leads to an increase in activity against Aspergillus fumigatus. Introduction of an alpha-methyl group has a marked additional beneficial effect. Investigation of pyridinyl and pyrimidinyl analogues resulted in the identification of 30 (UK-109,496, voriconazole) which has excellent potency against a broad range of fungal pathogens including A. fumigatus and Candida krusei. Copyright (C) 1996 Elsevier Science Ltd.

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页码：2031 / 2036

页数：6

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