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Bioorg Med Chem Lett. 2009 Sep 1;19(17):5128-31. doi: 10.1016/j.bmcl.2009.07.029. Epub 2009 Jul 10.

Antiparasitic activities of novel, orally available fumagillin analogs.

Author information

1
Praecis Pharmaceuticals, 830 Winter Street, Waltham, MA 02451, USA. christopher.c.arico-muendel@gsk.com

Abstract

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.

PMID:
19648008
PMCID:
PMC2745105
DOI:
10.1016/j.bmcl.2009.07.029
[Indexed for MEDLINE]
Free PMC Article

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