Evaluation of Diarylureas for Activity Against Plasmodium falciparum

A library of diarylurea insulin-like growth factor 1 receptor inhibitors was screened for activity against chloroquine-sensitive (3D7) and chloroquine-resistant (K1) strains of Plasmodium falciparum. The 4-aminoquinaldine-derived diarylureas displayed promising antimalarial potency. Further explorat...

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Published in:ACS medicinal chemistry letters 2010-12, Vol.1 (9), p.460-465
Main Authors: Zhang, Yiqun, Anderson, Marc, Weisman, Jennifer L, Lu, Min, Choy, Cindy J, Boyd, Vincent A, Price, Jeanine, Sigal, Martina, Clark, Julie, Connelly, Michele, Zhu, Fangyi, Guiguemde, W. Armand, Jeffries, Cynthia, Yang, Lei, Lemoff, Andrew, Liou, Ally P, Webb, Thomas R, DeRisi, Joseph L, Guy, R. Kiplin
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Language:English
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Summary:A library of diarylurea insulin-like growth factor 1 receptor inhibitors was screened for activity against chloroquine-sensitive (3D7) and chloroquine-resistant (K1) strains of Plasmodium falciparum. The 4-aminoquinaldine-derived diarylureas displayed promising antimalarial potency. Further exploration of the B ring of 4-aminoquinaldinyl ureas allowed identification of several quinaldin-4-yl ureas 4{13, 39} and 4{13, 58} sufficiently potent against both 3D7 and K1 strains to qualify as bone fide leads.
ISSN:1948-5875
1948-5875
DOI:10.1021/ml100083c