Literature DB >> 19410451

The discovery of a structurally novel class of inhibitors of the type 1 glycine transporter.

John A Lowe1, Xinjun Hou, Christopher Schmidt, F David Tingley, Stan McHardy, Monica Kalman, Shari Deninno, Mark Sanner, Karen Ward, Lorraine Lebel, Don Tunucci, James Valentine, Brian S Bronk, Eric Schaeffer.   

Abstract

The type 1 glycine transporter plays an important in regulating homeostatic glycine levels in the brain that are relevant to the activation of the NMDA receptor by the excitatory neurotransmitter glutamate. We describe herein the structure-activity relationships (SAR) of a structurally novel class of GlyT1 inhibitors following on a lead derived from high throughput screening, which shows good selectivity for GlyT1 and potent activity in elevating CSF levels of glycine.

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Year:  2009        PMID： 19410451     DOI： 10.1016/j.bmcl.2009.04.035

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  2 in total

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

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
Journal:  Bioorg Med Chem Lett       Date:  2014-01-13       Impact factor: 2.823

2.  Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: development of a [3.3.0]-based series and other piperidine bioisosteres.

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
Journal:  Bioorg Med Chem Lett       Date:  2014-01-13       Impact factor: 2.823
  2 in total

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