Quinoxaline NN′-dioxide derivatives and related compounds as growth inhibitors of Trypanosoma cruzi.: Structure-activity YP relationships

被引：83

作者：

Aguirre, G

Cerecetto, H

Di Maio, R

González, M

Alfaro, MEM

Jaso, A

Zarranz, B

Ortega, MA

Aldana, I

Monge-Vega, A

机构：

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

[2] Univ Nacl Mayor San Marcos, Fac Farm & Bioquim, Lab Invest Patentes & Desarrollo, Lima, Peru

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 14期

关键词：

Trypanosoma cruzi; growth inhibitors; anti-parasitic agents;

D O I：

10.1016/j.bmcl.2004.04.088

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Quinoxaline derivatives presented good inhibitor activity of growth of Trypanosoma cruzi in in vitro assays. The 50% inhibitory doses were of the same order of that of Nifurtimox. Derivative 13, a quinoxaline N,N'-dioxide derivative, and the reduced derivatives 19 and 20 were the most cytotoxic compounds against the protozoan. Structural requirements for optimal activity were studied by computational methods. From statistical analysis we could establish a multiple correlation between activity and lipophilic properties and LUMO energy. (C) 2004 Elsevier Ltd. All rights reserved.

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页码：3835 / 3839

页数：5

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