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Praziquantel derivatives exhibit activity against both juvenile and adult Schistosoma japonicum

  作者 Duan, WW; Qiu, SJ; Zhao, Y; Sun, HA; Qiao, CH; Xia, CM  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-4;  页码  1587-1590  
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[摘要]A praziquantel analog 10-hydroxy praziquantel and eight praziquantel/peroxide conjugates were synthesized. The biological activity of these compounds was evaluated against juvenile and adult stages of Schistosoma japonicum. Unlike praziquantel, 10-hydroxy praziquantel exhibits activity against both juvenile and adult Schistosoma japonicumin. All hybrid compounds displayed modest to significant worm killing activity. The present study has important significance for the development of hybrid antischistosomal drugs. Crown Copyright (C) 2012 Published by Elsevier Ltd. All rights reserved.

 
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