1564262-49-2Relevant academic research and scientific papers
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: Development of a potent and CNS penetrant [3.1.0]-based lead
Jones, Carrie K.,Sheffler, Douglas J.,Williams, Richard,Jadhav, Sataya B.,Felts, Andrew S.,Morrison, Ryan D.,Niswender, Colleen M.,Daniels, J. Scott,Conn, P. Jeffrey,Lindsley, Craig W.
, p. 1067 - 1070 (2014/03/21)
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 preclinical model of schizophrenia (prepulse inhibition).
