Abstract
Inhibition of the sodium hydrogen exchanger isoform-1 (NHE-1) has been shown to limit damage to the myocardium under ischemic conditions in animals. While most known NHE-1 inhibitors are acylguanidines, this report describes the design and synthesis of a series of heterocyclic inhibitors of NHE-1 including aminoimidazoles with undiminished in vitro activity and oral bioavailability.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Administration, Oral
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Biological Availability
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Cation Transport Proteins / antagonists & inhibitors*
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Cation Transport Proteins / metabolism
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Cell Line
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Guanidines / administration & dosage*
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Guanidines / chemistry
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Guanidines / pharmacokinetics
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Humans
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Imidazoles / administration & dosage*
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Imidazoles / chemistry
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Imidazoles / pharmacokinetics
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Membrane Proteins / antagonists & inhibitors*
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Membrane Proteins / metabolism
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Protein Isoforms / antagonists & inhibitors
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Protein Isoforms / metabolism
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Sodium-Hydrogen Exchanger 1
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Sodium-Hydrogen Exchangers / antagonists & inhibitors*
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Sodium-Hydrogen Exchangers / metabolism
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Stereoisomerism
Substances
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Cation Transport Proteins
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Guanidines
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Imidazoles
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Membrane Proteins
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Protein Isoforms
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SLC9A1 protein, human
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Sodium-Hydrogen Exchanger 1
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Sodium-Hydrogen Exchangers