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Design and Synthesis of Novel Pyrazole‐based Lp‐PLA 2 Inhibitors
Author(s) -
Wang Yi,
Xu Weiren,
Shao Hua,
Xie Yafei,
Wang Jianwu
Publication year - 2011
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.201180354
Subject(s) - chemistry , pyrazole , in vitro , combinatorial chemistry , lipoprotein associated phospholipase a2 , stereochemistry , biological activity , phospholipase a2 , biochemistry , enzyme
Abstract A series of novel pyrazole‐based lipoprotein‐associated phospholipase A 2 (Lp‐PLA 2 ) inhibitors have been designed and synthetized by a variety of acetophenones via a 10‐step convergent approach. The synthetic approach is carefully optimized, and an unsuccessful alternative route is also discussed. The in vitro biological activity reveals that all the synthesized compounds are potent Lp‐PLA 2 inhibitors with compound 13b being the most potent one (Lp‐PLA 2 , IC 50 =1.5 nmol/L).