title: Design, synthesis, and SAR of N-((1-(4-(propylsulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1.
abstract: The design, synthesis, and structure-activity relationships (SAR) of a series of N-((1-(4-(propylsulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1 (GlyT-1) are described. Optimization of the benzamide and central ring components of the core scaffold led to the identification of a GlyT-1 inhibitor that demonstrated in vivo activity in a rodent cerebral spinal fluid (CSF) glycine model.
authors: AMRI, 26 Corporate Circle, PO Box 15098, Albany, NY 12212-5098, USA. christopher.cioffi@amriglobal.com
authors: Christopher L
authors: CL
authors: Cioffi
authors: Mark A
authors: MA
authors: Wolf
authors: Peter R
authors: PR
authors: Guzzo
authors: Kashinath
authors: K
authors: Sadalapure
authors: Visweswaran
authors: V
authors: Parthasarathy
authors: Dattatraya
authors: D
authors: Dethe
authors: Jun-Ho
authors: JH
authors: Maeng
authors: Edmund
authors: E
authors: Carulli
authors: David T J
authors: DT
authors: Loong
authors: Xiao
authors: X
authors: Fang
authors: Min
authors: M
authors: Hu
authors: Priya
authors: P
authors: Gupta
authors: Mark
authors: M
authors: Chung
authors: Mei
authors: M
authors: Bai
authors: Nick
authors: N
authors: Moore
authors: Michele
authors: M
authors: Luche
authors: Yuri
authors: Y
authors: Khmelnitsky
authors: Patrick L
authors: PL
authors: Love
authors: Megan A
authors: MA
authors: Watson
authors: Andrew J
authors: AJ
authors: Mhyre
authors: Shuang
authors: S
authors: Liu
mesh_terms: D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D005998:Glycine / Q000134:cerebrospinal fluid; D050487:Glycine Plasma Membrane Transport Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D057809:HEK293 Cells; D006801:Humans; D008862:Microsomes, Liver / Q000378:metabolism; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D001549:Benzamides; D050487:Glycine Plasma Membrane Transport Proteins; D010879:Piperazines; D005998:Glycine