Novel antiprotozoal products:: Imidazole and benzimidazole N-oxide derivatives and related compounds

被引：82

作者：

Aguirre, G

Bolani, M

Cerecetto, H

Gerpe, A

González, M

Sainz, YF

Denicola, A

de Ocáriz, CO

Nogal, JJ

Montero, D

Escario, JA

机构：

[1] Univ Republica, Dept Quim Organ, Fac Quim, Montevideo 11400, Uruguay

[2] Univ Republica, Dept Quim Organ, Fac Ciencias, Montevideo 11400, Uruguay

[3] Univ Burgos, Fac Ciencias, Burgos, Spain

[4] Fac Ciencias, Lab Fisicoquim Biol, Montevideo, Uruguay

[5] CSIC, Inst Quim Med, E-28006 Madrid, Spain

[6] Univ Complutense Madrid, Fac Farm, Dept Parasitol, Madrid, Spain

来源：

ARCHIV DER PHARMAZIE | 2004年 / 337卷 / 05期

关键词：

anti-protozoa compounds; imidazole N-oxide; structure-activity relationship;

D O I：

10.1002/ardp.200300840

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The syntheses and biological evaluation of the first anti-protozoa imidazole N-oxide and benzimidazole N-oxide and their derivatives are reported. They were tested in vitro against two different protozoa, Trypanosoma cruzi and Trichomonas vaginalis. Derivative 7c, ethyl- 1 -(i-butyloxycarbonyloxy)-6-nitrobenzimidazole-2-carboxylate, displayed activity on both protozoa. Lipophilicity and redox potential were experimentally determined in order to study the relationship with activity of the compounds. These properties are well related with the observed bioactivity. Imidazole and benzimidazole N-oxide derivatives are becoming leaders for further chemical modifications and advanced biological studies.

引用

页码：259 / 270

页数：12

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