Bioorganic & Medicinal Chemistry Letters 2006-12-01

Synthesis and SAR of GlyT1 inhibitors derived from a series of N-((4-(morpholine-4-carbonyl)-1-(propylsulfonyl)piperidin-4-yl)methyl)benzamides.

Zhijian Zhao, Julie A O'Brien, Wei Lemaire, David L Williams, Marlene A Jacobson, Cyrille Sur, Doug J Pettibone, Philip R Tiller, Sheri Smith, George D Hartman, Scott E Wolkenberg, Craig W Lindsley

Index: Bioorg. Med. Chem. Lett. 16(23) , 5968-72, (2006)

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Abstract

This Letter describes the synthesis and SAR, developed through an iterative analog library approach, of potent and selective non-sarcosine-derived GlyT1 inhibitors.