1-Benzylbenzimidazoles: the discovery of a novel series of bradykinin B1 receptor antagonists

Guo, Qin ; Chandrasekhar, Jayaraman ; Ihle, David ; Wustrow, David J. ; Chenard, Bertrand L. ; Krause, James E. ; Hutchison, Alan ; Alderman, Dawn ; Cheng, Charles ; Cortright, Daniel ; Broom, Daniel ; Kershaw, Mark T. ; Simmermacher-Mayer, Jean ; Peng, Yao ; Hodgetts, Kevin J. (2008) 1-Benzylbenzimidazoles: the discovery of a novel series of bradykinin B1 receptor antagonists Bioorganic & Medicinal Chemistry Letters, 18 (18). pp. 5027-5031. ISSN 0960-894X

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Official URL: http://linkinghub.elsevier.com/retrieve/pii/S09608...

Related URL: http://dx.doi.org/10.1016/j.bmcl.2008.08.014

Abstract

The design, synthesis, and structure-activity studies of a novel series of BK B1 receptor antagonists based on a 1-benzylbenzimidazole chemotype are described. A number of compounds, for example, 38g, with excellent affinity for the cynomolgus macaque and rat bradykinin B1 receptor were discovered.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:Bradykinin B; P-glycoprotein; 1-Benzylbenzimidazole
ID Code:7181
Deposited On:25 Oct 2010 12:20
Last Modified:04 Feb 2011 04:45

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