Bisphosphonates derived from fatty acids are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase

被引:72
作者
Szajnman, SH
Montalvetti, A
Wang, YH
Docampo, R
Rodriguez, JB
机构
[1] Univ Buenos Aires, Fac Ciencias Exactas & Nat, Dept Quim Organ, RA-1428 Buenos Aires, DF, Argentina
[2] Univ Illinois, Mol Parasitol Lab, Dept Pathobiol, Urbana, IL 61802 USA
[3] Univ Illinois, Ctr Zoonoses Res, Urbana, IL 61802 USA
关键词
D O I
10.1016/S0960-894X(03)00663-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Studies on the mode of action of a series of bisphosphonates derived from fatty acids, which had previously proved to be potent inhibitors against Trypanosoma cruzi proliferation in in vitro assays, have been performed. Some of these drugs proved to be potent inhibitors against the intracellular form of the parasite, exhibiting IC50 values at the low micromolar level. As bisphosphonates are FDA clinically approved for treatment of bone resorption disorders, their potential innocuousness makes them good candidates to control tropical diseases. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3231 / 3235
页数:5
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