Bioorganic & medicinal chemistry letters, 2009-09, Vol.19 (18), p.5334-5338
2009
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Details
- Autor(en) / Beteiligte
- Titel
- Discovery of isoxazole voltage gated sodium channel blockers for treatment of chronic pain
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2009-09, Vol.19 (18), p.5334-5338
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2009
- Quelle
- Access via ScienceDirect (Elsevier)
- Beschreibungen/Notizen
- 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 v1.7 inhibitory potency. The spirocyclobutyl substitution had the most significant enhancement on Na v1.7 inhibitory activity.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2009.07.135Titel-ID: cdi_proquest_miscellaneous_734014527
- Format
- –
- Schlagworte
- Amide replacement, Analgesics, Animals, Biological and medical sciences, Cell Line, Chronic Disease, Heterocycles, Humans, Inflammatory pain, Isoxazole, Isoxazoles - chemistry, Isoxazoles - pharmacology, Isoxazoles - therapeutic use, Medical sciences, Neuropathic pain, Neuropharmacology, Pain - drug therapy, Pain - immunology, Pharmacology. Drug treatments, Rats, Sodium Channel Blockers - chemistry, Sodium Channel Blockers - pharmacology, Sodium Channel Blockers - therapeutic use, Sodium Channels - metabolism, Spinal Nerves - drug effects, Structure-Activity Relationship, Voltage gated sodium channel blocker