Abstract
A series of carbo- and heterocyclic alpha-hydroxy amide-derived bradykinin B1 antagonists was prepared and evaluated. A 4,4-difluorocyclohexyl alpha-hydroxy amide was incorporated along with a 2-methyl tetrazole in lieu of an oxadiazole to afford a suitable compound with good pharmacokinetic properties, CNS penetration, and clearance by multiple metabolic pathways.
MeSH terms
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Amides / chemical synthesis*
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Amides / chemistry
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Amides / pharmacokinetics
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Amides / pharmacology*
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Animals
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Bradykinin B1 Receptor Antagonists*
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Central Nervous System / drug effects
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Combinatorial Chemistry Techniques
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Drug Design
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Humans
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Molecular Structure
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Rats
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Structure-Activity Relationship
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Tetrazoles / chemical synthesis*
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Tetrazoles / chemistry
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Tetrazoles / pharmacokinetics
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Tetrazoles / pharmacology*
Substances
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Amides
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Bradykinin B1 Receptor Antagonists
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Tetrazoles