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ID: ALA1154006
Journal: Bioorg Med Chem Lett
Title: Optimisation of a series of potent, selective and orally bioavailable GlyT1 inhibitors.
Authors: Thomson JL, Blackaby WP, Jennings AS, Goodacre SC, Pike A, Thomas S, Brown TA, Smith A, Pillai G, Street LJ, Lewis RT.
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.
CiteXplore: 19318248