title: Synthesis and SAR of GlyT1 inhibitors derived from a series of N-((4-(morpholine-4-carbonyl)-1-(propylsulfonyl)piperidin-4-yl)methyl)benzamides.
abstract: This Letter describes the synthesis and SAR, developed through an iterative analog library approach, of potent and selective non-sarcosine-derived GlyT1 inhibitors.
authors.affiliation: Department of Medicinal Chemistry, Merck and Co., Inc., PO Box 4, West Point, PA 19486, USA. zhijian_zhao@merck.com <zhijian_zhao@merck.com>
authors.forename: Zhijian
authors.initials: Z
authors.lastname: Zhao
authors.forename: Julie A
authors.initials: JA
authors.lastname: O'Brien
authors.forename: Wei
authors.initials: W
authors.lastname: Lemaire
authors.forename: David L
authors.initials: DL
authors.lastname: Williams
authors.forename: Marlene A
authors.initials: MA
authors.lastname: Jacobson
authors.forename: Cyrille
authors.initials: C
authors.lastname: Sur
authors.forename: Doug J
authors.initials: DJ
authors.lastname: Pettibone
authors.forename: Philip R
authors.initials: PR
authors.lastname: Tiller
authors.forename: Sheri
authors.initials: S
authors.lastname: Smith
authors.forename: George D
authors.initials: GD
authors.lastname: Hartman
authors.forename: Scott E
authors.initials: SE
authors.lastname: Wolkenberg
authors.forename: Craig W
authors.initials: CW
authors.lastname: Lindsley
mesh_terms: D000577:Amides / Q000737:chemistry; D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D050487:Glycine Plasma Membrane Transport Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D008745:Methylation; D051379:Mice; D015394:Molecular Structure; D009025:Morpholines / Q000737:chemistry*; D010880:Piperidines / Q000737:chemistry*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D001549:Benzamides; D050487:Glycine Plasma Membrane Transport Proteins; D009025:Morpholines; D010880:Piperidines; C032727:piperidine