| Literature DB >> 23149228 |
Robert M Rzasa1, Essa Hu, Shannon Rumfelt, Ning Chen, Kristin L Andrews, Samer Chmait, James R Falsey, Wenge Zhong, Adrie D Jones, Amy Porter, Steven W Louie, Xiaoning Zhao, James J S Treanor, Jennifer R Allen.
Abstract
We report the discovery of a novel series of biaryl ethers as potent and selective PDE10A inhibitors. Structure-activity studies improved the potency and decreased Pgp-mediated efflux found in the initial compound 4. X-ray crystallographic studies revealed two novel binding modes to the catalytic site of the PDE10A enzyme.Entities:
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Year: 2012 PMID： 23149228 DOI： 10.1016/j.bmcl.2012.10.078
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823