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

doi:10.1016/j.bmcl.2014.01.013

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 journal › Article › peer-review

11 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 language	English
Pages (from-to)	1067-1070
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	24
Issue number	5
Early online date	13 Jan 2014
DOIs	https://doi.org/10.1016/j.bmcl.2014.01.013
Publication status	Published - 15 Feb 2014

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http://www.sciencedirect.com/science/article/pii/S0960894X14000328#

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Jones, C. K., Sheffler, D. J., Williams, R., Jadhav, S. B., Felts, A. S., Morrison, R. D., Niswender, C. M., Daniels, J. S., & Conn, P. J. (2014). Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: Development of a potent and CNS penetrant [3.1.0]-based lead. Bioorganic and Medicinal Chemistry Letters, 24(5), 1067-1070. https://doi.org/10.1016/j.bmcl.2014.01.013

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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). ",

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AU - Jones, Carrie K.

AU - Sheffler, Douglas J.

AU - Williams, Richard

AU - Jadhav, Sataya B.

AU - Felts, Andrew S.

AU - Morrison, Ryan D.

AU - Niswender, Colleen M.

AU - Daniels, J. Scott

AU - Conn, P. Jeffrey

PY - 2014/2/15

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AB - 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).

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DO - 10.1016/j.bmcl.2014.01.013

M3 - Article

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SP - 1067

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 5

ER -

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

Abstract

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