Bradykinin B1 antagonists: SAR studies in the 2,3-diaminopyridine series
SAR study of the biphenyl region of 2,3-diaminopyridine bradykinin B 1 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 B 1 receptor.
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.