Phenol‐benzoxazolone bioisosteres of GluN2B‐NMDA receptor antagonists: Unexpected rearrangement during reductive alkylation with phenylcyclohexanone
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DOI: 10.1002/ardp.202200225
Abstract: Negative allosteric modulators of N‐methyl‐ d‐aspartate receptors containing the GluN2B subunit represent promising drug candidates for the treatment of various neurological disorders including stroke, epilepsy, and Parkinson's disease. To increase the bioavailability and GluN2B affinity,… read more here.
Keywords: benzoxazolone bioisosteres; phenol benzoxazolone; phenol; glun2b nmda ... See more keywords
Ifenprodil Stereoisomers: Synthesis, Absolute Configuration, and Correlation with Biological Activity.
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DOI: 10.1021/acs.jmedchem.0c01912
Abstract: Ifenprodil (1) is a potent GluN2B-selective N-methyl-d-aspartate (NMDA) receptor antagonist that is used as a cerebral vasodilator and has been examined in clinical trials for the treatment of drug addiction, idiopathic pulmonary fibrosis, and COVID-19.… read more here.
Keywords: configuration; ifenprodil; ifenprodil stereoisomers; glun2b nmda ... See more keywords
Chemical, pharmacodynamic and pharmacokinetic characterization of the GluN2B receptor antagonist 3-(4-phenylbutyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-1,7-diol – starting point for PET tracer development
Sign Up to like & getrecommendations! Published in 2022 at "Biological Chemistry"
DOI: 10.1515/hsz-2022-0222
Abstract: Abstract GluN2B-NMDA receptors play a key role in several neurological and neurodegenerative disorders. In order to develop novel negative allosteric GluN2B-NMDA receptor modulators, the concept of conformational restriction was pursued, i.e. the flexible aminoethanol substructure… read more here.
Keywords: glun2b; benzazepine diol; tetrahydro benzazepine; glun2b nmda ... See more keywords