个性化文献订阅>期刊> Journal of Medicinal Chemistry
 

Lead Optimization of Antimalarial Propafenone Analogues

  作者 LOWES DAVID; PRADHAN ANUPAM; IYER LALITHA V; PARMAN TOUFAN; GOW JASON; ZHU FANGYI; FURIMSKY ANNA; LEMOFF ANDREW; GUIGUEMDE W ARMAND; SIGAL MARTINA; CLARK JULIE A; WILSON EMILY; TANG LIANG; CONNELLY MICHELE C; DERISI JOSEPH L; KYLE DENNIS E; MIRSALIS JON; GUY R KIPLIN  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2012年55-13;  页码  6087-6093  
  关联知识点  
 

[摘要]Previously reported studies identified analogues of propafenone that had potent antimalarial activity, reduced cardiac ion channel activity, and properties that suggested the potential for clinical development for malaria. Careful examination of the bioavailability, pharmacokinetics, toxicology, and efficacy of this series of compounds using rodent models revealed orally bioavailable compounds that are nontoxic and suppress parasitemia in vivo. Although these compounds possess potential for further preclinical development, they also carry some significant challenges.

 
      被申请数(0)  
 

[全文传递流程]

一般上传文献全文的时限在1个工作日内