Synthesis of quinolinyl chalcones and evaluation of their antimalarial activity

被引：168

作者：

Domínguez, JN ^{[1
]}

Charris, JE

Lobo, G

de Domínguez, NG

Moreno, MM

Riggione, F

Sanchez, E

Olson, J

Rosenthal, PJ

机构：

[1] Cent Univ Venezuela, Fac Farm, Lab Sintesis Organ, Caracas 1051, Venezuela

[2] Cent Univ Venezuela, Fac Farm, Lab Bioquim, Caracas 1051, Venezuela

[3] Cent Univ Venezuela, Fac Med, Lab Invest Malaria, Caracas 1051, Venezuela

[4] Univ Carabobo, Lab Inmunoparasitol Biomed, Maracay, Venezuela

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

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2001年 / 36卷 / 06期

关键词：

antimalarial; falcipain; synthesis; chalcones; P; berghei; falciparum;

D O I：

10.1016/S0223-5234(01)01245-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Quinolinyl chalcones were synthesized and evaluated for their inhibition of the Plasmodium falciparum cystein protease falcipain and their activity against cultured P. falciparum parasites. They were also tested for in vivo efficacy in a rodent P. berghei model. Their activity against falcipain and as antimalarials was moderate, but antimalarial activity was probably not due to the inhibition of falcipain and may follow a different mechanism. 1-(2,4-Dichlorophenyl)-3-[3-(2-chloro-6,7-dimethoxiquinolinyl)]-2-propen-1-one 3j was the most promising compound among those here reported (IC50 19.0 muM). (C) 2001 Editions scientifiques et medicales Elsevier SAS.

引用

页码：555 / 560

页数：6

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