Abstract
Modification of the structure of bosentan 1, the first marketed endothelin receptor antagonist (Tracleer), by introduction of a second sulfonamide function at the alkoxy side chain, led to bis-sulfonamides 2. This allowed to prepare dual ET(A)/ET(B) as well as ET(B) receptor selective antagonists, which could serve as tools to investigate the pharmacological consequences of selective ET(B) receptor blockade.
MeSH terms
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Animals
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Aorta / drug effects
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Aorta / physiology
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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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Inhibitory Concentration 50
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Muscle, Smooth, Vascular / drug effects
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Muscle, Smooth, Vascular / physiology
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Rats
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Receptors, Endothelin / metabolism
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Structure-Activity Relationship
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Sulfonamides / chemistry*
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Sulfonamides / pharmacology*
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Vasoconstriction / drug effects
Substances
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Endothelin Receptor Antagonists
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Receptors, Endothelin
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Sulfonamides