Abstract
A novel series of Oxytocin antagonists are described. This series was identified through pharmacophoric overlap of in-house and literature antagonists. Subsequent optimization led to a series of potent, selective antagonists. Several analogues displayed oral bioavailability in vivo in the rat.
MeSH terms
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Administration, Oral
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Animals
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Combinatorial Chemistry Techniques
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Molecular Structure
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Oxytocics / chemical synthesis
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Oxytocics / chemistry
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Oxytocics / pharmacokinetics
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Oxytocics / pharmacology*
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Oxytocin / antagonists & inhibitors*
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Rats
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Structure-Activity Relationship
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Triazoles / chemical synthesis*
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Triazoles / chemistry
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Triazoles / pharmacokinetics
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Triazoles / pharmacology*
Substances
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Oxytocics
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Triazoles
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Oxytocin