Phenol—Benzoxazolone bioisosteres: Synthesis and biological evaluation of tricyclic GluN2B‐selective N‐methyl‐ d‐aspartate receptor antagonists
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DOI: 10.1002/ardp.202200147
Abstract: Tricyclic tetrahydrooxazolo[4,5‐h]‐[3]benzazepin‐9‐ols 22 were designed as phenol bioisosteres of tetrahydro‐3‐benzazepine‐1,7‐diols. Key features of the synthesis are the introduction of the trifluoromethylsulfonyl and allyl protective groups at the heterocyclic N‐atoms. Two methods were developed to convert… read more here.
Keywords: bioisosteres synthesis; glun2b; benzoxazolone bioisosteres; phenol benzoxazolone ... See more keywords
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