Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10587924 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
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.
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Authors
Christopher L. Cioffi, Mark A. Wolf, Peter R. Guzzo, Kashinath Sadalapure, Visweswaran Parthasarathy, Dattatraya Dethe, Jun-Ho Maeng, Edmund Carulli, David T.J. Loong, Xiao Fang, Min Hu, Priya Gupta, Mark Chung, Mei Bai, Nick Moore, Michele Luche,