| Literature DB >> 19648008 |
Christopher Arico-Muendel1, Paolo A Centrella, Brooke D Contonio, Barry A Morgan, Gary O'Donovan, Christopher L Paradise, Steven R Skinner, Barbara Sluboski, Jennifer L Svendsen, Kerry F White, Anjan Debnath, Jiri Gut, Nathan Wilson, James H McKerrow, Joseph L DeRisi, Philip J Rosenthal, Peter K Chiang.
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.Entities:
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Year: 2009 PMID： 19648008 PMCID： PMC2745105 DOI： 10.1016/j.bmcl.2009.07.029
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823