Design and synthesis of novel α-aminoamides derivatives as Nav1.7 inhibitors for antinociception was written by Xue, Dengqi;Liu, Yani;Zheng, Yilin;Niu, Heling;Dong, Liying;Ouyang, Xiangshuo;Song, Siyu;Zhang, Denggao;Ge, Qianwei;Wang, Kewei;Shao, Liming. And the article was included in Chinese Chemical Letters in 2022.Formula: C8H9FO This article mentions the following:
Three novel series of α-aminoamides derivatives were designed and synthesized based on ralfinamide, and their Nav1.7 inhibitory activities were evaluated using manual patch clamp electrophysiol. Active compounds inhibited Nav1.7 with half maximal inhibitory concentration (IC50) values ranging from 2.9μmol/L to 21.4μmol/L. Among them, the most potent compound I [R = 2H-1,3-benzodioxol-4-ylmethyl] exhibited about 12-fold potency better than ralfinamide. The investigation of their structure-activity relationship gives a strategy to improve the Nav1.7 inhibition of ralfinamide analogs. Compound I [R = 2H-1,3-benzodioxol-4-ylmethyl] was efficacious in antinociception in the mouse spared nerve injury (SNI) model of neuropathic pain without causing sedation in the open field test. In the experiment, the researchers used many compounds, for example, (S)-1-(2-Fluorophenyl)ethanol (cas: 171032-87-4Formula: C8H9FO).
(S)-1-(2-Fluorophenyl)ethanol (cas: 171032-87-4) belongs to alcohols. Because alcohols are easily synthesized and easily transformed into other compounds, they serve as important intermediates in organic synthesis. The most common reactions of alcohols can be classified as oxidation, dehydration, substitution, esterification, and reactions of alkoxides.Formula: C8H9FO
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts