Synthesis and Bioactivity of Substituted Benzoylguanidine Derivatives as Potent Na + /H +  Exchanger Inhibitors | Zendy

Jin Ning | Zendy; Yang Yun | Zendy; Xu Wenting | Zendy; Yang Xiaozhi | Zendy; Gong Guoqing | Zendy; Xu Yungen | Zendy

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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.

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