期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 17, 页码 5128-5131出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.07.029
关键词
MetAP2; Fumagillin; TNP-470; Antiparasitic; Malaria; Trypanosomes; Amoeba; PPI-2458
资金
- The Sandler Foundation
- NIH [U01-AI53862]
Fumagillin, an irreversible inhibitor of MetAP2, has been shown to potently inhibit growth of malaria parasites in vitro. Here, we demonstrate activity of fumagillin analogs with an improved pharmacokinetic profile against malaria parasites, trypanosomes, and amoebas. A subset of the compounds showed efficacy in a murine malaria model. The observed SAR forms a basis for further optimization of fumagillin based inhibitors against parasitic targets by inhibition of MetAP2. (C) 2009 Elsevier Ltd. All rights reserved.
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