Synthesis and Evaluation of Novel α-Aminoamides Containing Benzoheterocyclic Moiety for the Treatment of Pain
oleh: Kun Tong, Ruotian Zhang, Fengzhi Ren, Tao Zhang, Junlin He, Jingchao Cheng, Zixing Yu, Fengxia Ren, Yatong Zhang, Weiguo Shi
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2021-03-01 |
Deskripsi
Novel α-aminoamide derivatives containing different benzoheterocyclics moiety were synthesized and evaluated as voltage-gated sodium ion channels blocks the treatment of pain. Compounds <b>6a</b>, <b>6e</b>, and <b>6f</b> 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<sub>v</sub>1.7 and anti-Na<sub>v</sub>1.8 activity in the patch-clamp electrophysiology assay. Therefore, compounds <b>6a</b>, <b>6e</b>, and <b>6f</b>, which have inhibitory potency for two pain-related Na<sub>v</sub> targets, could serve as new leads for the development of analgesic medicines.