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

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 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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10.1016/j.bmcl.2014.01.013

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

Jones, Carrie K. ; Sheffler, Douglas J. ; Williams, Richard ; Jadhav, Sataya B. ; Felts, Andrew S. ; Morrison, Ryan D. ; Niswender, Colleen M. ; Daniels, J. Scott ; Conn, P. Jeffrey. / Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: Development of a potent and CNS penetrant [3.1.0]-based lead. In: Bioorganic and Medicinal Chemistry Letters. 2014 ; Vol. 24, No. 5. pp. 1067-1070.

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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). ",

author = "Jones, {Carrie K.} and Sheffler, {Douglas J.} and Richard Williams and Jadhav, {Sataya B.} and Felts, {Andrew S.} and Morrison, {Ryan D.} and Niswender, {Colleen M.} and Daniels, {J. Scott} and Conn, {P. Jeffrey}",

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Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: Development of a potent and CNS penetrant [3.1.0]-based lead. / Jones, Carrie K.; Sheffler, Douglas J.; Williams, Richard; Jadhav, Sataya B.; Felts, Andrew S.; Morrison, Ryan D.; Niswender, Colleen M.; Daniels, J. Scott; Conn, P. Jeffrey.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 24, No. 5, 15.02.2014, p. 1067-1070.

Research output: Contribution to journal › Article › peer-review

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AU - Conn, P. Jeffrey

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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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