Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10587079 | Bioorganic & Medicinal Chemistry Letters | 2014 | 4 Pages |
Abstract
This Letter describes the development and SAR of a novel series of GlyT1 inhibitors derived from a scaffold hopping approach that provided a robust intellectual property position, in lieu of a traditional, expensive HTS campaign. Members within this new [3.1.0]-based series displayed excellent GlyT1 potency, selectivity, free fraction, CNS penetration and efficacy in a preclinical model of schizophrenia (prepulse inhibition).
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Authors
Carrie K. Jones, Douglas J. Sheffler, Richard Williams, Sataya B. Jadhav, Andrew S. Felts, Ryan D. Morrison, Colleen M. Niswender, J. Scott Daniels, P. Jeffrey Conn, Craig W. Lindsley,