| Literature DB >> 16870426 |
Xiaozhang Zheng1, Kevin J Hodgetts, Harry Brielmann, Alan Hutchison, Frank Burkamp, A Brian Jones, Peter Blurton, Robert Clarkson, Jayaraman Chandrasekhar, Rajagopal Bakthavatchalam, Stéphane De Lombaert, Marci Crandall, Daniel Cortright, Charles A Blum.
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.Entities:
Mesh：
Substances：
Year: 2006 PMID： 16870426 DOI： 10.1016/j.bmcl.2006.07.010
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823