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Praziquantel Derivatives with Antischistosomal Activity: Aromatic Ring Modification
Author(s) -
Wang Zhixia,
Chen Jinglei,
Qiao Chunhua
Publication year - 2013
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12153
Subject(s) - praziquantel , in vivo , chemistry , ring (chemistry) , in vitro , pharmacology , stereochemistry , combinatorial chemistry , biology , organic chemistry , schistosomiasis , biochemistry , helminths , immunology , microbiology and biotechnology
A series of aromatic ring‐modified praziquantel derivatives were prepared and evaluated against juvenile and adult stage of S chistosoma japonicumin . Several analogs comparable in activity to the drug praziquantel have been identified based on in vitro and in vivo japonuicum schistosomes worm viability assay. Structure and activity relationship of these praziquantel aromatic ring‐modified compounds was revealed. Specifically, a compound in which a bromine has been introduced in the aromatic ring of praziquantel demonstrated close antischistosomal activity to praziquantel in vivo .