Design, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes)

被引:30
作者
Schvartzapel, AJ
Zhong, L
Docampo, R
Rodriguez, JB
Gros, EG
机构
[1] UNIV BUENOS AIRES,FAC CIENCIAS EXACTAS & NAT,DEPT QUIM ORGAN,RA-1428 BUENOS AIRES,DF,ARGENTINA
[2] UNIV ILLINOIS,COLL VET MED,DEPT PATHOBIOL,MOL PARASITOL LAB,URBANA,IL 61801
关键词
D O I
10.1021/jm9607616
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
As a continuation of our project aimed at the search for new chemotherapeutic agents against Chagas' disease, several drugs structurally related to the insect growth regulator Fenoxycarb and the naturally occurring juvenile hormone of insects were designed, synthesized, and evaluated as antiproliferative agents against the parasite responsible of this disease. Isoprenoid derivatives (compounds 33, 34, 36, and 37) were potent growth inhibitors of Trypanosoma cruzi epimastigotes. In addition, taking into account the high activity observed for compound 30 and the inhibitory action of related compounds, the allyl ether moiety bonded at the polar extreme of these inhibitors proved to be a promising group for the design of new drugs.
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收藏
页码:2314 / 2322
页数:9
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