Abstract
SAR study of the biphenyl region of 2,3-diaminopyridine bradykinin B1 antagonists was investigated with non-aromatic carbo- and heterocyclic rings. A piperidine ring was found to be a good replacement for the proximal phenyl ring while replacement of the distal phenyl was optimal with a cyclohexyl group leading to a dramatic improvement in affinity for the B1 receptor.
MeSH terms
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Aminopyridines / chemical synthesis*
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Aminopyridines / pharmacokinetics
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Aminopyridines / pharmacology
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Animals
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Bradykinin / antagonists & inhibitors
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Bradykinin B1 Receptor Antagonists*
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Humans
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Pharmacokinetics
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Protein Binding
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Rats
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Rats, Sprague-Dawley
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Structure-Activity Relationship
Substances
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Aminopyridines
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Bradykinin B1 Receptor Antagonists
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2,3-diaminopyridine
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Bradykinin