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Discovery and SAR studies of novel GlyT1 inhibitors |
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| Authors: | Walter Magnus W Hoffman Beth J Gordon Kimberly Johnson Kirk Love Patrick Jones Matthew Man Teresa Phebus Lee Reel Jon K Rudyk Helene C Shannon Harlan Svensson Kjell Yu Hong Valli Matthew J Porter Warren J |
| Institution: | Lilly Research Laboratories, Eli Lilly and Company, Erl Wood Manor, Windlesham, Surrey GU20 6PH, UK. magnus.walter@lilly.com |
| Abstract: | Inhibition of the glycine transporter GlyT1 is a potential strategy for the treatment of schizophrenia. A novel series of GlyT1 inhibitors and their structure-activity relationships (SAR) are described. Members of this series are highly potent and selective transport inhibitors which are shown to elevate glycine levels in cerebrospinal fluid. |
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