Abstract
A number of 4'-heterocyclic biphenylsulfonamide derivatives, formally derived from BMS-193884 (1) by replacing the oxazole ring with other heterocyclic rings, are potent and selective endothelin A (ET(A)) receptor antagonists. Among the analogues examined, the pyrimidine derivative 18 is the most potent (K(i)=0.9 nM) and selective for the ET(A) receptor, approximately equivalent to 1.
MeSH terms
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Animals
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Biphenyl Compounds / chemical synthesis*
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Biphenyl Compounds / chemistry
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Biphenyl Compounds / pharmacology
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CHO Cells
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Cricetinae
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Endothelin Receptor Antagonists*
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Humans
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Protein Binding
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Receptor, Endothelin A
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Receptors, Endothelin / genetics
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Receptors, Endothelin / metabolism
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Sulfonamides / chemistry
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Sulfonamides / pharmacology
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Transfection
Substances
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Biphenyl Compounds
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Endothelin Receptor Antagonists
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Receptor, Endothelin A
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Receptors, Endothelin
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Sulfonamides