- Synthesis of Kappa Opioid Antagonists Based on Pyrrolo[1,2-α]quinoxalinones Using an N-Arylation/Condensation/Oxidation Reaction Sequence
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The quinoxaline and quinoxalinone family of nitrogen heterocycles is present in molecules of therapeutic relevance for diverse applications ranging from infectious diseases to neuroscience targets. Here, we describe a general synthetic sequence to afford pyrrolo[1,2-α]quinoxalinones from commercially available starting materials and their use in preparing potential kappa opioid receptor antagonists. The biological data obtained from the latter set of compounds is briefly presented and discussed.
- Scarry, Sarah M.,Lovell, Kimberly M.,Frankowski, Kevin J.,Bohn, Laura M.,Aubé, Jeffrey
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p. 10538 - 10550
(2016/11/17)
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- KAPPA OPIOID RECEPTOR EFFECTORS AND USES THEREOF
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The present invention is a selective kappa opioid receptor effector, or a pharmaceutically acceptable salt thereof, useful for treating ethanol use disorder withdrawal, anxiety and/or depression, schizophrenia, mania or post-traumatic stress disorder.
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Paragraph 00053
(2013/03/28)
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