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Synthesis of Perspicamide A and Related Diverse Analogues: Their Bioevaluation as Potent Antileishmanial Agents

  作者 PANDEY ANAND KUMAR; SHARMA RASHMI; SHIVAHARE RAHUL; ARORA ASHISH; RASTOGI NEERAJ; GUPTA SUMAN; CHAUHAN PREM M S  
  选自 期刊  Journal of Organic Chemistry;  卷期  2013年78-4;  页码  1534-1546  
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[摘要]The first protocol for the synthesis of perspicamide A and related diverse analogues has been developed from economical and readily available starting materials. Furthermore, a few synthesized analogues, 24a, 246, 24c, 24d, and 241, exhibited potent activity against Leishmania donovani with IC50 values ranging from 3.75 to 10.37 mu M and a selectivity index (SI) ranging from 9.58 to 53.12, which is improved compared to the standard drug Miltefosine (IC50 12.4 mu M and SI 4.1).

 
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