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Optimisation of a series of potent,selective and orally bioavailable GlyT1 inhibitors |
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| Authors: | Joanne L Thomson Wesley P Blackaby Andrew SR Jennings Simon C Goodacre Andrew Pike Steve Thomas Terry A Brown Alison Smith Gopalan Pillai Leslie J Street Richard T Lewis |
| Institution: | Department of Medicinal Chemistry, Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK |
| Abstract: | A series of heterocyclic sulfonamides have been developed which are potent and selective inhibitors of hGlyT1. SAR studies to optimise the in vitro and in vivo properties are described. Optimisation of the central scaffold resulted in cyclohexane sulfones 28 and 29, which have good PK properties and show promise for further development. |
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