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Bioorg Med Chem Lett. 2012 Dec 15;22(24):7371-5. doi: 10.1016/j.bmcl.2012.10.078. Epub 2012 Oct 22.

Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux.

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  • 1Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320-1799, USA. rrzasa@amgen.com


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.

Copyright © 2012 Elsevier Ltd. All rights reserved.

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