Literature DB >> 19181525

Discovery of GlyT1 inhibitors with improved pharmacokinetic properties.

Scott E Wolkenberg1, Zhijian Zhao, David D Wisnoski, William H Leister, Julie O'Brien, Wei Lemaire, David L Williams, Marlene A Jacobson, Cyrille Sur, Gene G Kinney, Doug J Pettibone, Philip R Tiller, Sheri Smith, Christopher Gibson, Bennett K Ma, Stacey L Polsky-Fisher, Craig W Lindsley, George D Hartman.   

Abstract

Glycine transporter 1 (GlyT1) represents a novel target for the treatment of schizophrenia via the potentiation of glutamatergic NMDA receptors. The discovery of 4,4-disubstituted piperidine inhibitors of GlyT1 which exhibit improved pharmacokinetic properties, including oral bioavailability, is discussed.

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Year:  2009        PMID： 19181525     DOI： 10.1016/j.bmcl.2009.01.015

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


  5 in total

1.  Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1.

Authors:  Wesley P Blackaby; Richard T Lewis; Joanne L Thomson; Andrew S R Jennings; Simon C Goodacre; Leslie J Street; Angus M MacLeod; Andrew Pike; Suzanne Wood; Steve Thomas; Terry A Brown; Alison Smith; Gopalan Pillai; Sarah Almond; Martin R Guscott; H Donald Burns; Waisi Eng; Christine Ryan; Jacquelynn Cook; Terence G Hamill
Journal:  ACS Med Chem Lett       Date:  2010-06-25       Impact factor: 4.345

2.  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

3.  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

4.  Glycine transporter-1 inhibition promotes striatal axon sprouting via NMDA receptors in dopamine neurons.

Authors:  Yvonne Schmitz; Candace Castagna; Ana Mrejeru; José E Lizardi-Ortiz; Zoe Klein; Craig W Lindsley; David Sulzer
Journal:  J Neurosci       Date:  2013-10-16       Impact factor: 6.167

5.  Glutamatergic targets for enhancing extinction learning in drug addiction.

Authors:  R M Cleva; J T Gass; J J Widholm; M F Olive
Journal:  Curr Neuropharmacol       Date:  2010-12       Impact factor: 7.363
  5 in total

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