Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10587076 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
Abstract
This Letter describes the development and SAR of a novel series of GlyT1 inhibitors derived from a scaffold hopping approach, in lieu of an HTS campaign, which provided intellectual property position. Members within this new [3.3.0]-based series displayed excellent GlyT1 potency, selectivity, free fraction, and modest CNS penetration. Moreover, enantioselective GlyT1 inhibition was observed, within this novel series and a number of other piperidine bioisosteric cores.
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Authors
Douglas J. Sheffler, Michael T. Nedelcovych, Richard Williams, Stephen C. Turner, Brittany B. Duerk, Megan R. Robbins, Sataya B. Jadhav, Colleen M. Niswender, Carrie K. Jones, P. Jeffrey Conn, R. Nathan Daniels, Craig W. Lindsley,