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5-Piperazinyl pyridine carboxamide bradykinin B1 antagonists |
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| Authors: | Kuduk Scott D Di Marco Christina Ng Chang Ronald K Wood Michael R Kim June J Schirripa Kathy M Murphy Kathy L Ransom Richard W Tang Cuyue Torrent Maricel Ha Sookhee Prueksaritanont Thomayant Pettibone Douglas J Bock Mark G |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA. scott_d_kuduk@merck.com |
| Abstract: | A series of 2,3-diaminopyridine bradykinin B(1) antagonists was modified to mitigate the potential for bioactivation. Removal of the 3-amino group and incorporation of basic 5-piperazinyl carboxamides at the pyridine 5-position provided compounds with high affinity for the human B(1) receptor. |
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