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吡喹酮衍生物对日本血吸虫的幼体和成虫均有活性。

Praziquantel derivatives exhibit activity against both juvenile and adult Schistosoma japonicum.

机构信息

College of Pharmaceutical Science, Soochow University, Suzhou, China.

出版信息

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1587-90. doi: 10.1016/j.bmcl.2011.12.133. Epub 2012 Jan 4.

Abstract

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.

摘要

合成了一种吡喹酮类似物 10-羟基吡喹酮和 8 种吡喹酮/过氧化物缀合物。评价了这些化合物对日本血吸虫幼体和成虫的生物活性。与吡喹酮不同,10-羟基吡喹酮对日本血吸虫的幼体和成虫均有活性。所有杂交化合物均显示出适度至显著的杀蠕虫活性。本研究对开发杂交抗血吸虫药物具有重要意义。

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