1373427-95-2Relevant academic research and scientific papers
Synthesis and bioactivity of substituted benzoylguanidine derivatives as potent Na+/H+ exchanger inhibitors
Jin, Ning,Yang, Yun,Xu, Wenting,Yang, Xiaozhi,Gong, Guoqing,Xu, Yungen
, p. 333 - 340 (2012/05/19)
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 IC50 value of 1.08 × 10-10 molmiddot;L-1, was 39 times more potent than lead compound CPU-X-050420 in vitro tests. A novel series of 5-(2-(4-(2,3,4-trimethoxybenzyl)piperazin-1-yl)acetyl)benzoylguanidine derivatives 6a-6i have been synthesized and screened for their NHE1 inhibitory activity. Copyright
