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Discovery of isoxazole voltage gated sodium channel blockers for treatment of chronic pain
- Source :
- Bioorganic & Medicinal Chemistry Letters. 19:5334-5338
- Publication Year :
- 2009
- Publisher :
- Elsevier BV, 2009.
-
Abstract
- A series of novel isoxazole voltage gated sodium channel blockers have been synthesized and evaluated. Substitutions on the benzylic position of benzamide were investigated to determine their effect on Na(v)1.7 inhibitory potency. The spirocyclobutyl substitution had the most significant enhancement on Na(v)1.7 inhibitory activity.
- Subjects :
- medicine.drug_class
Stereochemistry
Clinical Biochemistry
Analgesic
Pain
Pharmaceutical Science
Carboxamide
Pharmacology
Inhibitory postsynaptic potential
Biochemistry
Sodium Channels
Cell Line
Structure-Activity Relationship
chemistry.chemical_compound
Sodium channel blocker
Drug Discovery
medicine
Animals
Humans
Structure–activity relationship
Isoxazole
Voltage-Gated Sodium Channel Blockers
Benzamide
Molecular Biology
Chemistry
Organic Chemistry
Isoxazoles
Rats
Spinal Nerves
Chronic Disease
Molecular Medicine
Sodium Channel Blockers
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 19
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....701dc8af84f883465fcabf2285c21877
- Full Text :
- https://doi.org/10.1016/j.bmcl.2009.07.135