Praziquantel derivatives exhibit activity against both juvenile and adult Schistosoma japonicum

被引：33
|
作者：
Duan, Wen-wen [1 ]
Qiu, Si-jie [2 ]
Zhao, Yue [1 ]
Sun, Huan [2 ]
Qiao, Chunhua [1 ]
Xia, Chao-ming [2 ]
机构：
[1] Soochow Univ, Coll Pharmaceut Sci, Suzhou 215123, Peoples R China
[2] Soochow Univ, Dept Parasitol, Suzhou 215123, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 04期
关键词：
Praziquantel derivatives; Antischistosomal; Hybrid drugs; Schistosoma japonicum; SYNTHETIC TRIOXOLANES; IN-VITRO; CHEMOTHERAPY; MANSONI; FUTURE;
D O I：
10.1016/j.bmcl.2011.12.133
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
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.
引用
收藏
页码：1587 / 1590
页数：4
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