Abstract
A series of 4-substituted (benzo[b]thiophene-2-carbonyl)guanidines was synthesized and evaluated for the NHE-1 inhibitory activity and cardioprotective efficacy both in vitro and in vivo. Several analogs exhibited a strong inhibition on NHE-1, and which was generally well correlated with their cardioprotective efficacy. Especially the 4-nitro 20 and cyano 50 compounds excellently improved the cardiac function and reduced infarct size against ischemia/reperfusion injury.
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 Pressure / drug effects
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Cardiotonic Agents / chemical synthesis
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Cardiotonic Agents / chemistry
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Cardiotonic Agents / pharmacology*
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Guanidines / chemical synthesis
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Guanidines / chemistry
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Guanidines / pharmacology*
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In Vitro Techniques
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Myocardial Infarction / drug therapy
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Myocardial Ischemia / drug therapy*
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Myocardial Reperfusion Injury / drug therapy*
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Protein Isoforms / antagonists & inhibitors
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Rats
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Sodium-Hydrogen Exchangers / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Cardiotonic Agents
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Enzyme Inhibitors
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Guanidines
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Protein Isoforms
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Sodium-Hydrogen Exchangers