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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >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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Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na(+)/H(+) exchanger inhibitors, synthesis and protection against ischemic-reperfusion injury.

机译:苯并咪唑-2-基或苯并咪唑-2-基硫代甲基苯甲酰胍作为新型Na(+)/ H(+)交换剂抑制剂,合成和针对缺血再灌注损伤的保护作用。

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摘要

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.
机译:设计并合成了一系列新型的苯并咪唑-2-基或苯并咪唑-2-基硫甲基苯甲酰胍作为Na(+)/ H(+)交换抑制剂。发现它们中的大多数以浓度依赖的方式抑制NHE1介导的血小板肿胀,并对心肌缺血再灌注损伤具有显着的心脏保护作用,其中化合物10a和34在体内和体外均比卡立哌利德更有效。测试。

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