Literature DB >> 24900853

3-Amido-3-aryl-piperidines: A Novel Class of Potent, Selective, and Orally Active GlyT1 Inhibitors.

Emmanuel Pinard1, Daniela Alberati1, Ruben Alvarez-Sanchez1, Virginie Brom1, Serge Burner1, Holger Fischer1, Nicole Hauser1, Sabine Kolczewski1, Judith Lengyel1, Roland Mory1, Christian Saladin1, Tanja Schulz-Gasch1, Henri Stalder1.   

Abstract

3-Amido-3-aryl-piperidines were discovered as a novel structural class of GlyT1 inhibitors. The structure-activity relationship, which was developed, led to the identification of highly potent compounds exhibiting excellent selectivity against the GlyT2 isoform, drug-like properties, and in vivo activity after oral administration.

Entities:  

Keywords:  3-amido-3-aryl-piperidines; GlyT1 inhibitor; SAR; Schizophrenia

Year:  2014        PMID： 24900853      PMCID： PMC4027785          DOI： 10.1021/ml500005m

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  13 in total

Review 1.  N-methyl-d-aspartate (NMDA) receptor dysfunction or dysregulation: the final common pathway on the road to schizophrenia?

Authors:  Joshua T Kantrowitz; Daniel C Javitt
Journal:  Brain Res Bull       Date:  2010-04-24       Impact factor: 4.077

2.  Pharmacological evaluation of a novel assay for detecting glycine transporter 1 inhibitors and their antipsychotic potential.

Authors:  Daniela Alberati; Jean-Luc Moreau; Roland Mory; Emmanuel Pinard; Joseph G Wettstein
Journal:  Pharmacol Biochem Behav       Date:  2010-08-01       Impact factor: 3.533

3.  ALX 5407: a potent, selective inhibitor of the hGlyT1 glycine transporter.

Authors:  B N Atkinson; S C Bell; M De Vivo; L R Kowalski; S M Lechner; V I Ognyanov; C S Tham; C Tsai; J Jia; D Ashton; M A Klitenick
Journal:  Mol Pharmacol       Date:  2001-12       Impact factor: 4.436

4.  Glycine reuptake inhibitor RG1678: a pharmacologic characterization of an investigational agent for the treatment of schizophrenia.

Authors:  Daniela Alberati; Jean-Luc Moreau; Judith Lengyel; Nicole Hauser; Roland Mory; Edilio Borroni; Emmanuel Pinard; Frederic Knoflach; Götz Schlotterbeck; Dominik Hainzl; Joseph G Wettstein
Journal:  Neuropharmacology       Date:  2011-11-27       Impact factor: 5.250

5.  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

6.  Selective GlyT1 inhibitors: discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia.

Authors:  Emmanuel Pinard; Alexander Alanine; Daniela Alberati; Markus Bender; Edilio Borroni; Patrick Bourdeaux; Virginie Brom; Serge Burner; Holger Fischer; Dominik Hainzl; Remy Halm; Nicole Hauser; Synese Jolidon; Judith Lengyel; Hans-Peter Marty; Thierry Meyer; Jean-Luc Moreau; Roland Mory; Robert Narquizian; Mathias Nettekoven; Roger D Norcross; Bernd Puellmann; Philipp Schmid; Sebastien Schmitt; Henri Stalder; Roger Wermuth; Joseph G Wettstein; Daniel Zimmerli
Journal:  J Med Chem       Date:  2010-06-24       Impact factor: 7.446

Review 7.  Recent progress in the discovery of non-sarcosine based GlyT1 inhibitors.

Authors:  Scott E Wolkenberg; Cyrille Sur
Journal:  Curr Top Med Chem       Date:  2010       Impact factor: 3.295

8.  Tariquidar-induced P-glycoprotein inhibition at the rat blood-brain barrier studied with (R)-11C-verapamil and PET.

Authors:  Jens P Bankstahl; Claudia Kuntner; Aiman Abrahim; Rudolf Karch; Johann Stanek; Thomas Wanek; Wolfgang Wadsak; Kurt Kletter; Markus Müller; Wolfgang Löscher; Oliver Langer
Journal:  J Nucl Med       Date:  2008-07-16       Impact factor: 10.057

Review 9.  Glycine reuptake inhibition as a new therapeutic approach in schizophrenia: focus on the glycine transporter 1 (GlyT1).

Authors:  Pierre Chue
Journal:  Curr Pharm Des       Date:  2013       Impact factor: 3.116

10.  Glycine transport inhibitors for the treatment of schizophrenia.

Authors:  Kenji Hashimoto
Journal:  Open Med Chem J       Date:  2010-05-27
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  1 in total

Review 1.  Schizophrenia: synthetic strategies and recent advances in drug design.

Authors:  Maria Azmanova; Anaïs Pitto-Barry; Nicolas P E Barry
Journal:  Medchemcomm       Date:  2018-03-16       Impact factor: 3.597
  1 in total

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