Evaluation of Diarylureas for Activity Against Plasmodium falciparum.
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ABSTRACT:
SUBMITTER: Zhang Y
PROVIDER: S-EPMC3019604 | biostudies-literature | 2010 Dec
REPOSITORIES: biostudies-literature
Publications
Evaluation of Diarylureas for Activity Against Plasmodium falciparum.
Zhang Yiqun Y Anderson Marc M Weisman Jennifer L JL Lu Min M Choy Cindy J CJ Boyd Vincent A VA Price Jeanine J Sigal Martina M Clark Julie J Connelly Michele M Zhu Fangyi F Guiguemde W Armand WA Jeffries Cynthia C Yang Lei L Lemoff Andrew A Liou Ally P AP Webb Thomas R TR Derisi Joseph L JL Guy R Kiplin RK
ACS medicinal chemistry letters 20101201 9
A library of diarylurea IGFR 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. ...[more]
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