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Synthesis and Bioactivity of Substituted Benzoylguanidine Derivatives as Potent Na + /H + Exchanger Inhibitors
Author(s) -
Jin Ning,
Yang Yun,
Xu Wenting,
Yang Xiaozhi,
Gong Guoqing,
Xu Yungen
Publication year - 2012
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.201180470
Subject(s) - chemistry , in vitro , lead compound , inhibitory postsynaptic potential , medicinal chemistry , ic50 , sodium–hydrogen antiporter , stereochemistry , sodium , organic chemistry , biochemistry , neuroscience , biology
A novel series of substituted benzoylguanidine derivatives were designed and synthesized in order to evaluate their NHE1 inhibitory activity. Most of them were found to inhibit NHE1‐mediated platelet swelling in a concentration‐dependent manner, and eight compounds showed more potent NHE1 inhibitory activity than Cariporide. Compound 6f with an IC 50 value of 1.08×10 −10 mol·L −1 , was 39 times more potent than lead compound CPU‐X‐050420 in vitro tests.