Discovery of a novel class of isoxazoline voltage gated sodium channel blockers

Analogs of the previously reported voltage gated sodium channel blocker CDA54 were prepared in which one of the amide functions was replaced with aromatic and non-aromatic heterocycles. Replacement of the amide with an aromatic heterocycle resulted in significant loss of sodium channel blocking acti...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-09, Vol.19 (18), p.5329-5333
Main Authors: Shao, Pengcheng P., Ye, Feng, Weber, Ann E., Li, Xiaohua, Lyons, Kathryn A., Parsons, William H., Garcia, Maria L., Priest, Birgit T., Smith, McHardy M., Felix, John P., Williams, Brande S., Kaczorowski, Gregory J., McGowan, Erin, Abbadie, Catherine, Martin, William J., McMasters, Daniel R., Gao, Ying-Duo
Format: Article
Language:English
Subjects:
Amide replacement
Analgesics
Animals
Biological and medical sciences
Heterocycles
Inflammatory pain
Isoxazoles - chemistry
Isoxazoles - pharmacology
Isoxazoles - therapeutic use
Isoxazoline
Medical sciences
Models, Molecular
Molecular Structure
Neuropathic pain
Neuropharmacology
Pain - drug therapy
Pharmacology. Drug treatments
Rats
Rats, Sprague-Dawley
Sodium Channel Blockers - chemistry
Sodium Channel Blockers - pharmacology
Sodium Channel Blockers - therapeutic use
Spinal Nerves - drug effects
Structure-Activity Relationship
Voltage gated sodium channel blocker
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Summary:Analogs of the previously reported voltage gated sodium channel blocker CDA54 were prepared in which one of the amide functions was replaced with aromatic and non-aromatic heterocycles. Replacement of the amide with an aromatic heterocycle resulted in significant loss of sodium channel blocking activity, while non-aromatic heterocycle replacements were well tolerated.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.07.125