573675-83-9Relevant articles and documents
Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists
Blum, Charles A.,Caldwell, Timothy,Zheng, Xiaozhang,Bakthavatchalam, Rajagopal,Capitosti, Scott,Brielmann, Harry,De Lombaert, Stéphane,Kershaw, Mark T.,Matson, David,Krause, James E.,Cortright, Daniel,Crandall, Marci,Martin, William J.,Murphy, Beth Ann,Boyce, Susan,Jones, A. Brian,Mason, Glenn,Rycroft, Wayne,Perrett, Helen,Conley, Rachael,Burnaby-Davies, Nicola,Chenard, Bertrand L.,Hodgetts, Kevin J.
experimental part, p. 3330 - 3348 (2010/09/07)
The transient receptor potential cation channel, subfamily V, member 1 (TRPV1) is a nonselective cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective antago
From arylureas to biarylamides to aminoquinazolines: Discovery of a novel, potent TRPV1 antagonist
Zheng, Xiaozhang,Hodgetts, Kevin J.,Brielmann, Harry,Hutchison, Alan,Burkamp, Frank,Brian Jones,Blurton, Peter,Clarkson, Robert,Chandrasekhar, Jayaraman,Bakthavatchalam, Rajagopal,De Lombaert, Stephane,Crandall, Marci,Cortright, Daniel,Blum, Charles A.
, p. 5217 - 5221 (2007/10/03)
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 anta
