Synthesis and characterization of a novel gamma-aminobutyric acid type A (GABA(A)) receptor ligand that combines outstanding metabolic stability, pharmacokinetics, and anxiolytic efficacy

1,4-Benzodiazepines are used in the treatment of anxiety disorders but have limited long term use due to adverse effects. HZ-166 (2) has been shown to have anxiolytic-like effects with reduced sedative/ataxic liabilities. A 1,3-oxazole KRM-II-81 (9) was discovered from a series of six bioisosteres w...

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Pubblicato in:J Med Chem
Autori principali: Poe, Michael M., Methuku, Kashi Reddy, Li, Guanguan, Verma, Ashwini R., Teske, Kelly A., Stafford, Douglas C., Arnold, Leggy A., Cramer, Jeffrey W., Jones, Timothy M., Cerne, Rok, Krambis, Michael J., Witkin, Jeffrey M., Jambrina, Enrique, Rehman, Sabah, Ernst, Margot, Cook, James M., Schkeryantz, Jeffrey M.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2016
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC5215686/
https://ncbi.nlm.nih.gov/pubmed/27933953
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b01332
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