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Carboxamides as Modulators of Sodium Channels
ACS Medicinal Chemistry Letters ( IF 4.2 ) Pub Date : 2020-12-01 , DOI: 10.1021/acsmedchemlett.0c00590
Benjamin E Blass 1
Affiliation  

R5, R6, and R7 are each independently H, halo, C1–C6 alkyl, C1–C6 haloalkyl, C1–C6 alkoxy, or C1–C6 haloalkoxy; and R8 is C1–C6 alkyl; R5 is W-(CH2)n-Rz, C1–C6 alkylsulfanyl, -O-(CH2)p-Rw, or -O-(CH2)p-N(C1–C6alkyl)2; R6 and R7 are each independently H, halo, C1–C6 alkyl, C1–C6 haloalkyl, C1–C6 alkoxy, or C1–C6 haloalkoxy; and R8 is H; R5 and R6 are each independently H, halo, C1–C6 alkyl, C1–C6 haloalkyl, C1–C6 alkoxy, or C1–C6 haloalkoxy; R7 is W-(CH2)n-Rz, -C = C-Rx, or 3–6 membered cycloalkyl or phenyl, wherein said 3–6 membered cycloalkyl or phenyl is substituted with 1–3 substituents selected from a group consisting of C1–C6 alkoxy, CN, and -C(O)NH2; and R8 is H; or R5 is H, halo, C1–C6 alkyl, C1–C6 haloalkyl, C1–C6 alkoxy, or C1–C6 haloalkoxy; R6 and R7, together with the carbon atoms to which they are attached, form a ring of formula ; and R8 is H; Hameed, S. Nav 1.7 and Nav 1.8: Role in the pathophysiology of pain. Molecular Pain 2019, 15, 10.1177/2F1744806919858801 Han, C.; Huang, J.; Waxman, S. G. Sodium channel Nav 1.8: Emerging links to human disease. Neurology 2016, 86 (5), 473–483. Gilchrist, J.; Bosmans, F. Using voltage-sensor toxins and their molecular targets to investigate Nav1.8 gating. J. Physiol. 2018, 596 (10), 1863–1872. The author declares no competing financial interest. The author declares no competing financial interest. This article has not yet been cited by other publications.

中文翻译:

羧酰胺作为钠通道的调节剂

R 5、R 6和R 7各自独立地为H、卤素、C1-C6烷基、C1-C6卤代烷基、C1-C6烷氧基或C1-C6卤代烷氧基;R 8为C1-C6烷基;R 5是W-(CH 2 ) n -R z、C1-C6烷基硫烷基、-O-(CH 2 ) p -R w或-O-(CH 2 ) p -N(C1-C6烷基) 2;R 6和R 7各自独立地为H、卤素、C1-C6烷基、C1-C6卤代烷基、C1-C6烷氧基或C1-C6卤代烷氧基;R 8是H;R 5和 R 6各自独立地为 H、卤素、C1-C6 烷基、C1-C6 卤代烷基、C1-C6 烷氧基或 C1-C6 卤代烷氧基;R 7为W-(CH 2 ) n -R z,-C=CR x,或3-6元环烷基或苯基,其中所述3-6元环烷基或苯基被1-3个选自下组的取代基取代C1-C6烷氧基、CN和-C(O)NH 2;R 8是H;或R 5是H、卤素、C1-C6烷基、C1-C6卤代烷基、C1-C6烷氧基或C1-C6卤代烷氧基;R 6和R 7与它们所连接的碳原子一起形成下式的环;R 8是H;哈米德,S.Na v 1.7 和 Na v 1.8:在疼痛病理生理学中的作用。分子痛 2019 , 15 , 10.1177/2F1744806919858801韩,C黄,J瓦克斯曼,SG钠通道 Na v 1.8:与人类疾病的新联系。神经病学 2016 年86(5),473-483。吉尔克里斯特,J博斯曼斯,F.使用电压传感器毒素及其分子靶标研究 Na v 1.8 门控。J.生理学。 2018 , 596 (10), 1863–1872。作者声明没有竞争性经济利益。作者声明没有竞争性经济利益。这篇文章还没有被其他出版物引用。
更新日期:2020-12-10
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