Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives

被引：228

作者：

Domínguez, JN

León, C

Rodrigues, J

de Domínguez, NG

Gut, J

Rosenthal, PJ

机构：

[1] Cent Univ Venezuela, Fac Farm, Lab Sintesis Organ, San Francisco, CA 94143 USA

[2] Cent Univ Venezuela, Fac Farm, Lab Bioquim, San Francisco, CA 94143 USA

[3] Univ Calif San Francisco, San Francisco Gen Hosp, Dept Med, San Francisco, CA 94143 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 10期

关键词：

D O I：

10.1021/jm058208o

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

Phenylurenyl chalcone derivatives have been synthesized and tested as inhibitors of in vitro development of a chloroquine-resistant strain of Plasmodium falciparum, activity of the cysteme protease falcipain-2, in vitro globin hydrolysis, beta-hematin formation, and murine Plasmodium berghei malaria. The most active antimalarial compound was 1-[3'-N'-(N'-phenylurenyl)phenyl]-3(3,4,5-trimethoxyphenyl)-2-propen-1-one 49, with an IC50 of 1.76 mu M for inhibition of P. falciparum development. Results suggest that chalcones exert their antimalarial activity via multiple mechanisms.

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收藏

页码：3654 / 3658

页数：5

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