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Bradykinin B1 receptor antagonists: an alpha-hydroxy amide with an improved metabolism profile |
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| Authors: | Kuduk Scott D Chang Ronald K Dipardo Robert M Di Marco Christina N Murphy Kathy L Ransom Richard W Reiss Duane R Tang Cuyue Prueksaritanont Thomayant Pettibone Douglas J Bock Mark G |
| Affiliation: | Department of Medicinal Chemistry, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA. scott_d_kuduk@merck.com |
| Abstract: | A series of carbo- and heterocyclic alpha-hydroxy amide-derived bradykinin B1 antagonists was prepared and evaluated. A 4,4-difluorocyclohexyl alpha-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. |
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