| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1363719 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
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.
Graphical abstractAnalogs of fumagillin were shown to inhibit growth of three parasites and possess activity in a mouse model of malaria.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Christopher Arico-Muendel, 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,