Synthesis and evaluation of new difluoromethyl azoles as antileishmanial agents

被引：80

作者：

Ferreira, Sabrina B. ^{[2
]}

Costa, Marilia S. ^{[1
]}

Boechat, Nubia ^{[3
]}

Bezerra, Romulo J. S. ^{[4
]}

Genestra, Marcelo S. ^{[4
]}

Canto-Cavalheiro, Marilene M. ^{[4
]}

Kover, Warner B. ^{[2
]}

Ferreira, Vitor F. ^{[1
]}

机构：

[1] Univ Fed Fluminense, Inst Quim, Dept Quim Organ, BR-24020 Niteroi, RJ, Brazil

[2] Univ Fed Rio de Janeiro, Inst Quim, Dept Quim Organ, BR-21949 Rio De Janeiro, RJ, Brazil

[3] Fundacao Oswaldo Cruz, Inst Tecn Farm, Dept Sintese Organ, BR-21041250 Rio De Janeiro, RJ, Brazil

[4] Fundacao Oswaldo Cruz, Inst Oswaldo Cruz, Dept Immunol, BR-21041250 Rio De Janeiro, RJ, Brazil

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 42卷 / 11-12期

关键词：

antileishmanial activity; difluoromethylation; imidazole; 1,2,3-triazole;

D O I：

10.1016/j.ejmech.2007.02.020

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several compounds of great pharmacological interest contain the triazole and imidazole rings. In order to find new drugs with antileishmanial activity we have synthesized and evaluated new imidazole and triazole compounds carrying either the carbaldehyde or the difluoromethylene functionalities against promastigote forms of Leishmania amazonensis. Among the compounds tested difluoromethylene azoles 4b and 8f have inhibited the parasite growth significantly. Our results show that the introduction of the difluoromethylene moieties has turned the inactive carbaldehydes into active antileishmanial compounds. (C) 2007 Elsevier Masson SAS. All rights reserved.

引用

页码：1388 / 1395

页数：8

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