2-Aminobenzophenones as a novel class of bradykinin B1 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

doi:10.1021/jm800199h

2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists

J Med Chem. 2008 Jul 10;51(13):3946-52. doi: 10.1021/jm800199h. Epub 2008 Jun 14.

Authors

Dai-Shi Su¹, 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

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA. daishi_su@merck.com

PMID: 18553956
DOI: 10.1021/jm800199h

Abstract

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.

MeSH terms

Amines / chemistry*
Animals
Benzophenones / chemical synthesis
Benzophenones / chemistry*
Benzophenones / pharmacology*
Bradykinin B1 Receptor Antagonists*
Cell Line
Dogs
Humans
Molecular Structure
Rats
Receptor, Bradykinin B1 / metabolism
Structure-Activity Relationship

Substances

Amines
Benzophenones
Bradykinin B1 Receptor Antagonists
Receptor, Bradykinin B1