1227065-95-3Relevant 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.
PYRAZINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS
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Page/Page column 108, (2010/06/15)
Pyrazine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
