Farnesyltransferase inhibitors inhibit the growth of malaria parasites in vitro and in vivo

被引:73
作者
Wiesner, J
Kettler, K
Sakowski, J
Ortmann, R
Katzin, AM
Kimura, EA
Silber, K
Klebe, G
Jomaa, H
Schlitzer, M
机构
[1] Univ Munich, Dept Pharm, Zentrum Pharmaforsch, D-81377 Munich, Germany
[2] Univ Giessen, Inst Biochem, D-35392 Giessen, Germany
[3] Univ Sao Paulo, Inst Ciencias Biomed, BR-05508900 Sao Paulo, Brazil
[4] Univ Marburg, Inst Pharmazeut Chem, D-35032 Marburg, Germany
关键词
drug design; enzyme inhibitors; farnesyltransferase; malaria; medicinal chemistry;
D O I
10.1002/anie.200351169
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The inhibition of farnesyltransferase was recently suggested as a new strategy for malaria therapy. A class of farnesyltransferase inhibitors such as 1 has been prepared which have in vivo activity in a murine malaria model. These inhibitors significantly reduce the farnesylation of parasite proteins.
引用
收藏
页码:251 / 254
页数:4
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