Abstract
In order to search for novel inhibitors of Na+/H+ exchanger isoform-1 (NHE-1), nine feruloylagmatine analogues were designed and synthesized from ferulic acid and agmatine. The structures of the synthesized compounds were confirmed by 1H NMR, 13C NMR and mass spectra, among which compounds 5f-5i were novel compounds. The results of preliminary pharmacological test showed that some of the compounds possessed strong NHE-1 inhibitory activity, among which compounds 5a, 5b and 6c were more potent than cariporide in NHE-1 inhibition.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Agmatine / analogs & derivatives*
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Agmatine / chemical synthesis
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Agmatine / chemistry
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Agmatine / pharmacology
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Animals
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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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Drug Design
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Female
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Male
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Molecular Structure
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Rats
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Rats, Sprague-Dawley
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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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Sodium-Hydrogen Exchangers
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feruloylagmatine
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growth factor-activatable Na-H exchanger NHE-1
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Agmatine