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