Abstract
Studies to discover novel, potent and selective oxytocin antagonists are reported. Combinatorial libraries designed to find novel replacements of fragments of oxytocin antagonist L-371,257, identified pyrimidine, thiazole, indole and benzofuran as potential alternatives to the benzoic acid moiety of L-371,257. Additional investigations identified indole and benzofuran derivatives with potent oxytocin antagonist activity.
MeSH terms
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Animals
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Benzofurans / chemical synthesis*
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Benzofurans / chemistry
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Benzofurans / pharmacokinetics
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Benzofurans / pharmacology
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Biological Availability
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Dogs
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Drug Design
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Humans
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Indoles / chemical synthesis*
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Indoles / chemistry
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Indoles / pharmacokinetics
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Indoles / pharmacology
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Kinetics
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Models, Molecular
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Molecular Conformation
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Oxytocin / antagonists & inhibitors*
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Receptors, Oxytocin / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Benzofurans
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Indoles
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Receptors, Oxytocin
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Oxytocin