Evaluation of diarylureas for activity against plasmodium falciparum

Yiqun Zhang, Marc Anderson, Jennifer L. Weisman, Min Lu, Cindy J. Choy, Vincent A. Boyd, Jeanine Price, Martina Sigal, Julie Clark, Michele Connelly, Fangyi Zhu, W. Armand Guiguemde, Cynthia Jeffries, Lei Yang, Andrew Lemoff, Ally P. Liou, Thomas R. Webb, Joseph L. Derisi, R. Kiplin Guy

Research output: Contribution to journalArticlepeer-review

27 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)460-465
Number of pages6
JournalACS Medicinal Chemistry Letters
Volume1
Issue number9
DOIs
StatePublished - Dec 9 2010

Keywords

  • Malaria
  • diarylurea

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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