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
