Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: Development of a potent and CNS penetrant [3.1.0]-based lead

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

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)

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 preclin. model of schizophrenia (prepulse inhibition)​.
Original languageEnglish
Pages (from-to)1067-1070
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume24
Issue number5
Early online date13 Jan 2014
DOIs
Publication statusPublished - 15 Feb 2014

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