1415050-22-4Relevant academic research and scientific papers
Discovery of selective biaryl ethers as PDE10A inhibitors: Improvement in potency and mitigation of Pgp-mediated efflux
Rzasa, Robert M.,Hu, Essa,Rumfelt, Shannon,Chen, Ning,Andrews, Kristin L.,Chmait, Samer,Falsey, James R.,Zhong, Wenge,Jones, Adrie D.,Porter, Amy,Louie, Steven W.,Zhao, Xiaoning,Treanor, James J.S.,Allen, Jennifer R.
, p. 7371 - 7375 (2013/02/21)
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.
