A novel series of substituted benzoylguanidine derivatives were designed and synthesized in order to evaluate their NHE 1 inhibitory activity. Most of them were found to inhibit NHE 1-mediated platelet swelling in a c...A novel series of substituted benzoylguanidine derivatives were designed and synthesized in order to evaluate their NHE 1 inhibitory activity. Most of them were found to inhibit NHE 1-mediated platelet swelling in a concentration-dependent manner, and eight compounds showed more potent NHE 1 inhibitory activity than Cariporide. Compound 6f with an IC50 value of 1.08 × 10-10 mol·L-1, was 39 times more potent than lead compound CPU-X-050420 in vitro tests.展开更多
基金This work was supported by the National Natural Science Foundation of China （No. 30672512）.
文摘A novel series of substituted benzoylguanidine derivatives were designed and synthesized in order to evaluate their NHE 1 inhibitory activity. Most of them were found to inhibit NHE 1-mediated platelet swelling in a concentration-dependent manner, and eight compounds showed more potent NHE 1 inhibitory activity than Cariporide. Compound 6f with an IC50 value of 1.08 × 10-10 mol·L-1, was 39 times more potent than lead compound CPU-X-050420 in vitro tests.
