Bis-vinyl selenides obtained via iron(iii) catalyzed addition of PhSeSePh to alkynes: synthesis and antinociceptive activity
作者:Glaubia Sartori、José S. S. Neto、Ana Paula Pesarico、Davi F. Back、Cristina W. Nogueira、Gilson Zeni
DOI:10.1039/c2ob27064a
日期:——
In the present study the synthesis and antinociceptive activity of bis-vinyl selenides, prepared via FeCl3 promoted reaction addition of diorganyl dichalcogenides to alkynes, is described. The pharmacological results demonstrated that bis-vinyl selenides 3a, 3d, 3h and 3t elicited antinociceptive effect in the mouse formalin test. The antinociceptive effects of bis-vinyl selenides are not sensitive to electronic effects of the substituents on the aromatic ring directly bonded to the selenium atom. Bis-vinyl selenides 3h and 3t were the most promising molecules for pharmacological purposes since these bis-vinyl selenides were effective in both phases of the formalin test and against edema. A single dose of bis-vinyl selenides 3a, 3d, 3h and 3t did not cause acute toxicity in mice.
本研究介绍了双乙烯基硒化物的合成和抗痛觉活性。双乙烯基硒化物是通过氯化铁促进二乙烯基二羰基化合物与炔类化合物的反应加成而制备的。药理学结果表明,双乙烯基硒化物 3a、3d、3h 和 3t 在小鼠福尔马林试验中具有抗痛觉作用。双乙烯基硒化物的抗痛觉作用对直接与硒原子结合的芳香环上的取代基的电子效应并不敏感。双乙烯基硒化物 3h 和 3t 是最有希望用于药理学目的的分子,因为这些双乙烯基硒化物对福尔马林试验的两个阶段和水肿都有效。单剂量双乙烯基硒化物 3a、3d、3h 和 3t 不会对小鼠造成急性毒性。