Author/Authors :
Scott D. Kuduk، نويسنده , , Ronald K. Chang، نويسنده , , Robert M. DiPardo، نويسنده , , Christina N. Di Marco، نويسنده , , Kathy L. Murphy، نويسنده , , Richard W. Ransom، نويسنده , , Duane R. Reiss، نويسنده , , Cuyue Tang، نويسنده , , Thomayant Prueksaritanont، نويسنده , , Douglas J. Pettibone، نويسنده , , Mark G. Bock، نويسنده ,
Abstract :
A series of carbo- and heterocyclic α-hydroxy amide-derived bradykinin B1 antagonists was prepared and evaluated. A 4,4-difluorocyclohexyl α-hydroxy amide was incorporated along with a 2-methyl tetrazole in lieu of an oxadiazole to afford a suitable compound with good pharmacokinetic properties, CNS penetration, and clearance by multiple metabolic pathways.
Keywords :
pain , tetrazole , GPCR , bradykinin
