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Evaluation of Diarylureas for Activity Against Plasmodium falciparum

  作者 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  
  选自 期刊  ACS Medicinal Chemistry Letters;  卷期  2010年1-9;  页码  460-465  
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[摘要]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.

 
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