title: Synthesis and Na+/H+ exchanger inhibitory activity of benzoylguanidine derivatives.
abstract: Twenty-two compounds of substituted benzoylguanidine derivatives were designed and synthesized as potent NHE1 inhibitors. Twelve compounds showed more potent NHE1 inhibitory activity than cariporide. The activities of compounds 7e, 7h and 7j (IC(50) = 0.073 ± 0.021, 0.084 ± 0.012 and 0.068 ± 0.021 nmol/L, respectively) were two orders of magnitude higher than that of cariporide (30.7 ± 2.5 nmol/L). Myocardial cells in vitro screening showed 7j had highlighted protective effect on cardiomyocytes subjected to hypoxia/reoxygenation. Thus it is valuable for further investigation.
authors: Department of Medicinal Chemistry, China Pharmaceutical University, Tongjiaxiang 24, Nanjing 210009, China.
authors: Lu
authors: L
authors: Jin
authors: Xiang-Min
authors: XM
authors: Jiang
authors: Ping
authors: P
authors: Du
authors: Jing
authors: J
authors: Xu
authors: Guo-Qing
authors: GQ
authors: Gong
authors: Qiu-Juan
authors: QJ
authors: Wang
authors: Yun-Gen
authors: YG
authors: Xu
mesh_terms: D000818:Animals; D002478:Cells, Cultured; D006146:Guanidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D051381:Rats; D017923:Sodium-Hydrogen Exchangers / Q000037:antagonists & inhibitors*
chemical_list: D006146:Guanidines; D017923:Sodium-Hydrogen Exchangers