含苯并杂环部分的新型α-氨基酰胺用于疼痛治疗的合成与评价
Synthesis and Evaluation of Novel α-Aminoamides Containing Benzoheterocyclic Moiety for the Treatment of Pain.
作者信息
Tong Kun, Zhang Ruotian, Ren Fengzhi, Zhang Tao, He Junlin, Cheng Jingchao, Yu Zixing, Ren Fengxia, Zhang Yatong, Shi Weiguo
机构信息
State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology & Toxicology, 27 Tai-Ping Road, Beijing 100850, China.
Hebei University of Science & Technology, 26 Yuxiang Street, Shijiazhuang City 050018, China.
出版信息
Molecules. 2021 Mar 19;26(6):1716. doi: 10.3390/molecules26061716.
Novel α-aminoamide derivatives containing different benzoheterocyclics moiety were synthesized and evaluated as voltage-gated sodium ion channels blocks the treatment of pain. Compounds , , and 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-Na1.7 and anti-Na1.8 activity in the patch-clamp electrophysiology assay. Therefore, compounds , , and , which have inhibitory potency for two pain-related Na targets, could serve as new leads for the development of analgesic medicines.
合成了含有不同苯并杂环部分的新型α-氨基酰胺衍生物，并评估其作为电压门控钠离子通道阻滞剂在疼痛治疗中的作用。在福尔马林试验和扭体试验中，含有苯并呋喃基团的化合物、和显示出比瑞芬太尼更强的体内镇痛活性。有趣的是，在膜片钳电生理试验中，它们还表现出强大的体外抗Na1.7和抗Na1.8活性。因此，对两个与疼痛相关的钠靶点具有抑制效力的化合物、和可作为开发镇痛药的新先导物。
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