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
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
Bioorg Med Chem Lett. 2009 Sep 15;19(18):5334-8. doi: 10.1016/j.bmcl.2009.07.135. Epub 2009 Aug 6.
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.
一系列新型异恶唑电压门控钠通道阻滞剂已被合成并评估。研究了苯甲酰胺苄基位置的取代情况，以确定其对Na(v)1.7抑制效力的影响。螺环丁基取代对Na(v)1.7抑制活性有最显著的增强作用。
