This Letter describes the development and SAR of a novel series of GlyT1 inhibitors derived from a scaffold hopping approach that provided a robust intellectual property position, in lieu of a traditional, expensive HTS campaign. Members within this new [3.1.0]-based series displayed excellent GlyT1 potency, selectivity, free fraction, CNS penetration and efficacy in a preclin. model of schizophrenia (prepulse inhibition).
|Number of pages||4|
|Journal||Bioorganic and Medicinal Chemistry Letters|
|Early online date||13 Jan 2014|
|Publication status||Published - 15 Feb 2014|