Article

Bradykinin B1 antagonists: SAR studies in the 2,3-diaminopyridine series.

Department of Medicinal Chemistry, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA.
Bioorganic & Medicinal Chemistry Letters (impact factor: 2.55). 10/2005; 15(17):3925-9. DOI:10.1016/j.bmcl.2005.05.133 pp.3925-9
Source: PubMed

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.

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Keywords

2,3-diaminopyridine bradykinin B1 antagonists
 
biphenyl region
 
dramatic improvement
 
heterocyclic rings
 
piperidine ring
 
proximal phenyl ring
 
SAR study