Synthesis and Evaluation of Novel α-Aminoamides Containing Benzoheterocyclic Moiety for the Treatment of Pain

Molecules

Ruotian Zhang¹  Yatong Zhang¹  Fengzhi Ren²  Fengxia Ren³  Zixing Yu³  Tao Zhang³  Junlin He³  Jingchao Cheng³  Weiguo Shi³  Kun Tong³ 

[1] Hebei University of Science & Technology, 26 Yuxiang street, Shijiazhuang City 050018, China;New Drug Research & Development Co., Ltd., North China Pharmaceutical Group Corporation, Shijiazhuang City 050015, China;State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology & Toxicology, 27 Tai-Ping Road, Beijing 100850, China;

关键词: α-aminoamides;    sodium channel blocker;    Na_v1.7;    Na_v1.8;    dual channel inhibitors;   

DOI  :  10.3390/molecules26061716

来源: DOAJ

【 摘 要 】

Novel α-aminoamide derivatives containing different benzoheterocyclics moiety were synthesized and evaluated as voltage-gated sodium ion channels blocks the treatment of pain. Compounds 6a, 6e, and 6f containing the benzofuran group displayed more potent in vivo analgesic activity than ralfinamide in both the formalin test and the writhing assay. Interestingly, they also exhibited potent in vitro anti-Na_v1.7 and anti-Na_v1.8 activity in the patch-clamp electrophysiology assay. Therefore, compounds 6a, 6e, and 6f, which have inhibitory potency for two pain-related Na_v targets, could serve as new leads for the development of analgesic medicines.

【 授权许可】

Unknown