Bradykinin B 1 antagonists: SAR studies in the 2, 3-diaminopyridine series

…, T Prueksaritanont, RM Freidinger, DJ Pettibone…

Index: Kuduk, Scott D.; Chang, Ronald K.; Ng, Christina; Murphy, Kathy L.; Ransom, Richard W.; Tang, Cuyue; Prueksaritanont, Thomayant; Freidinger, Roger M.; Pettibone, Douglas J.; Bock, Mark G. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 17 p. 3925 - 3929

Full Text: HTML

Citation Number: 18

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.