Abstract
4-({2-[Isobutyl(phenylsulfonyl)amino]-5-(trifluoromethyl)phenoxy}methyl)benzoic acid (1) is a functional PGE2 antagonist selective for EP1 receptor subtype. Analogs of 1, in which the phenyl-sulfonyl moiety has been replaced with more hydrophilic heteroarylsulfonyl moieties, exhibited more optimized antagonist activity, while some of them showed in vivo antagonist activity. Structure-activity relationship (SAR) studies are also presented.
MeSH terms
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Alprostadil / metabolism*
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Animals
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CHO Cells
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Chromatography, Thin Layer
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Cricetinae
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Dinoprostone / analogs & derivatives
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Dinoprostone / metabolism
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Dinoprostone / pharmacology
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Drug Design
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Female
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Humans
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Indicators and Reagents
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Oxidation-Reduction
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Rats
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Receptors, Prostaglandin E / antagonists & inhibitors*
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Sulfonamides / pharmacology*
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Urinary Bladder / drug effects
Substances
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Indicators and Reagents
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Receptors, Prostaglandin E
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Sulfonamides
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sulprostone
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Alprostadil
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Dinoprostone