Blum, Charles A. ; Zheng, Xiaozhang ; Brielmann, Harry ; Hodgetts, Kevin J. ; Bakthavatchalam, Rajagopal ; Chandrasekhar, Jayaraman ; Krause, James E. ; Cortright, Daniel ; Matson, David ; Crandall, Marci ; Ngo, Chu K. ; Fung, Lawrence ; Day, Marta ; Kershaw, Mark ; De Lombaert, Stephane ; Chenard, Bertrand L. (2008) Aminoquinazolines as TRPV1 antagonists: modulation of drug-like properties through the exploration of 2-position substitution Bioorganic & Medicinal Chemistry Letters, 18 (16). pp. 4573-4577. 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.2008.07.036
Abstract
A focused SAR exploration of the lead 4-aminoquinazoline TRPV1 antagonist 2 led to the discovery of compound 18. In rats, compound 18 is readily absorbed following oral dosing and demonstrates excellent in vivo potency and efficacy in an acute inflammatory pain model.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Elsevier Science. |
| Keywords: | TRPV1; Aminoquinazolines; Antagonists; VR1 |
| ID Code: | 7127 |
| Deposited On: | 25 Oct 2010 12:31 |
| Last Modified: | 04 Feb 2011 05:01 |
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