Bioorganic & Medicinal Chemistry Letters 2009-09-15

Discovery of isoxazole voltage gated sodium channel blockers for treatment of chronic pain.

Pengcheng P Shao, Feng Ye, Ann E Weber, Xiaohua Li, Kathryn A Lyons, William H Parsons, Maria L Garcia, Birgit T Priest, McHardy M Smith, John P Felix, Brande S Williams, Gregory J Kaczorowski, Erin McGowan, Catherine Abbadie, William J Martin, Daniel R McMasters, Ying-Duo Gao

文献索引：Bioorg. Med. Chem. Lett. 19(18) , 5334-8, (2009)

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摘要

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.