Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.

Michael R Wood,Kathy M Schirripa, June J Kim,Scott D Kuduk,Ronald K Chang,Christina N Di Marco, Robert M DiPardo,Bang-Lin Wan, Kathy L Murphy, Richard W Ransom, Raymond S L Chang,Marie A Holahan,Jacquelynn J Cook,Wei Lemaire,Scott D Mosser,Rodney A Bednar,Cuyue Tang,Thomayant Prueksaritanont,Audrey A Wallace,Qin Mei,Jian Yu, Dennis L Bohn, Frank C Clayton,Emily D Adarayn, Gary R Sitko,Yvonne M Leonard, Roger M Freidinger, Douglas J Pettibone,Mark G Bock

Bioorganic & medicinal chemistry letters（2008）

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摘要

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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