31 research outputs found
Selective Antagonism of mGluR5 Alters Sleep-Wake and Quantitative EEG and Ameliorates Behavioral Abnormalities in a Rodent Model of Traumatic Stress
Selective Antagonism of mGluR5 Alters Sleep-Wake and Quantitative EEG and Ameliorates Behavioral Abnormalities in a Rodent Model of Traumatic Stress
Glutamine Antagonist JHU-083 Normalizes Aberrant Hippocampal Glutaminase Activity and Improves Cognition in APOE4 Mice
Corrigendum to “Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: Development of a [3.3.0]-based series and other piperidine bioisosteres” [Bioorg. Med. Chem. Lett. 24 (2014) 1062–1066]
Prevention and treatment of HIV infection and cognitive disease in mice by innate immune responses
Sleep in PTSD: Conceptual model and novel directions in brain-based research and interventions
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: Development of a [3.3.0]-based series and other piperidine bioisosteres
This letter describes the development and SAR of a novel series of GlyT1 inhibitors derived from a scaffold hopping approach, in lieu of an HTS campaign, which provided intellectual property position. Members within this new [3.3.0]-based series displayed excellent GlyT1 potency, selectivity, free fraction, and modest CNS penetration. Moreover, enantioselective GlyT1 inhibition was observed, within this novel series and a number of other piperidine bioisosteric cores