From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist

Zheng, Xiaozhang ; Hodgetts, Kevin J. ; Brielmann, Harry ; Hutchison, Alan ; Burkamp, Frank ; Jones, A. Brian ; Blurton, Peter ; Clarkson, Robert ; Chandrasekhar, Jayaraman ; Bakthavatchalam, Rajagopal ; De Lombaert, Stephane ; Crandall, Marci ; Cortright, Daniel ; Blum, Charles A. (2006) From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist Bioorganic & Medicinal Chemistry Letters, 16 (19). pp. 5217-5221. ISSN 0960-894X

Full text not available from this repository.

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

Related URL: http://dx.doi.org/10.1016/j.bmcl.2006.07.010

Abstract

Bioisosteric replacement of piperazine with an aryl ring in lead VR1 antagonist 1 led to the biarylamide series. The development of B-ring SAR led to the conformationally constrained analog 70. The resulting aminoquinazoline 70 represents a novel VR1 antagonist with improved in vitro potency and oral bioavailability vs the analogous compounds from the lead series.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:VR1; TRPV1; Pain; Bioisostere; Quinazoline; Ureas; Antagonist
ID Code:7177
Deposited On:25 Oct 2010 12:23
Last Modified:04 Feb 2011 05:14

Repository Staff Only: item control page