Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Blood Platelets / drug effects
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Chemistry, Pharmaceutical / methods
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Drug Design
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Drug Evaluation, Preclinical
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Guanidines / chemistry
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Guanidines / pharmacology*
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Imidazoles / chemistry
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Imidazoles / pharmacology*
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Inhibitory Concentration 50
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Models, Chemical
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Molecular Conformation
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Rats
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Reperfusion Injury / drug therapy*
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Sodium-Hydrogen Exchangers / chemistry
Substances
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Guanidines
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Imidazoles
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Sodium-Hydrogen Exchangers
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imidazole