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N-(6,7-Dichloro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-N-alkylsulfonamides as peripherally restricted N-methyl-d-aspartate receptor antagonists for the treatment of pain
- Source :
- Bioorganic & Medicinal Chemistry Letters. 17:4599-4603
- Publication Year :
- 2007
- Publisher :
- Elsevier BV, 2007.
-
Abstract
- It has been hypothesized that peripherally restricted NMDA receptor antagonists may be effective analgesics for osteoarthritis pain. A class of novel quinoxalinedione atropisomers, first discovered for an NMDA receptor antagonist program for the treatment of stroke, was evaluated and further optimized with the goal of finding peripherally restricted NMDA receptor antagonists.
- Subjects :
- Models, Molecular
medicine.medical_specialty
Clinical Biochemistry
Analgesic
Pain
Pharmaceutical Science
Quinoxalinedione
Blood–brain barrier
Receptors, N-Methyl-D-Aspartate
Biochemistry
Chemical synthesis
Structure-Activity Relationship
chemistry.chemical_compound
Internal medicine
Drug Discovery
medicine
Animals
Molecular Biology
Analgesics
Sulfonamides
Atropisomer
Binding Sites
Molecular Structure
Organic Chemistry
Glutamate receptor
Antagonist
Rats
medicine.anatomical_structure
Endocrinology
nervous system
chemistry
Area Under Curve
Molecular Medicine
NMDA receptor
Protein Binding
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 17
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....4dcf8a8aa89569f777c79f4224db99ed
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.05.083