Bioorganic & Medicinal Chemistry Letters 2005-09-01

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

Scott D Kuduk, Ronald K Chang, Christina Ng, Kathy L Murphy, Richard W Ransom, Cuyue Tang, Thomayant Prueksaritanont, Roger M Freidinger, Douglas J Pettibone, Mark G Bock

Index: Bioorg. Med. Chem. Lett. 15(17) , 3925-9, (2005)

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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.