2-Aminobenzophenones As A Novel Class Of Bradykinin B-1 Receptor Antagonists

Dai-Shi Su,John L. Lim,Elizabeth Tinney,Bang-Lin Wan,Kathy L. Murphy,Duane R. Reiss,C. Meacham Harrell,Stacy S. O'Malley,Rick W. Ransom,Raymond S. L. Chang,Douglas J. Pettibone,Jian Yu,Cuyue Tang,Thomayant Prueksaritanont,Roger M. Freidinger,Mark G. Bock,Neville J. Anthony

JOURNAL OF MEDICINAL CHEMISTRY（2008）

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摘要

Selective bradykinin (BK) B-1 receptor antagonists could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure activity relationships of the structurally novel HTS lead compound 1 provided potent hBK B-1 receptor antagonists with excellent receptor occupancy in the CNS of hBK B-1 transgenic rats.

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