Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na+/H+ exchanger inhibitors, synthesis and protection against ischemic-reperfusion injury
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- 作者：Rui Zhang ; Lin Lei ; Yun-Gen Xu ; Wei-Yi Hua ; Guo-Qing Gong
- 关键词：Na+/H+ exchanger ; Na+/H+ exchanger inhibitors ; Myocardial ischemic-reperfusion injury ; Benzoylguanidine derivatives ; Synthesis
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 出版时间：1 May 2007
- 年：2007
- 卷：17
- 期：9
- 页码：2430-2433
- 全文大小：128 K
文摘
A novel series of benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines were designed and synthesized as Na+/H+exchanger inhibitors. Most of them were found to inhibit NHE1-mediated platelet swelling in a concentration-dependent manner, and to have significant cardioprotective effect against myocardial ischemic-reperfusion injury, among which compounds 10a and 34 were more potent than cariporide in both in vivo and in vitro tests.