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Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists |
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| Authors: | Wood Michael R Schirripa Kathy M Kim June J Kuduk Scott D Chang Ronald K Di Marco Christina N DiPardo Robert M Wan Bang-Lin Murphy Kathy L Ransom Richard W Chang Raymond S L Holahan Marie A Cook Jacquelynn J Lemaire Wei Mosser Scott D Bednar Rodney A Tang Cuyue Prueksaritanont Thomayant Wallace Audrey A Mei Qin Yu Jian Bohn Dennis L Clayton Frank C Adarayn Emily D Sitko Gary R Leonard Yvonne M Freidinger Roger M Pettibone Douglas J Bock Mark G |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA. michael_wood2@merck.com |
| Abstract: | Antagonism of the bradykinin B(1) receptor represents a potential treatment for chronic pain and inflammation. Novel antagonists incorporating alpha-hydroxy amides were designed that display low-nanomolar affinity for the human bradykinin B(1) receptor and good bioavailability in the rat and dog. In addition, these functionally active compounds show high passive permeability and low susceptibility to phosphoglycoprotein mediated efflux, predictive of good CNS exposure. |
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