Abstract

In the current study, new morpholine-linked thiazoles were prepared by the reaction of salicylaldehyde derivative, thiosemicarbazide, and α-bromoketones. To mediate the previous three-component reaction, the reaction was conducted using two equiv. of piperazine in dioxane at reflux for 5 h. Using the prior protocol, two series of thiazoles, linked to arene or chromene units, were prepared in good to excellent yields. The new thiazoles were examined as potential inhibitors of acetylcholinesterase at a concentration of 50 µM. When compared to donepezil (inhibition percentage of 92.8%), hybrids 11b and 11c, linked to 6-chloro or 6-bromochromen-3-yl units, gave the best inhibition percentages of 72.3 and 71.5%, respectively. Furthermore, when tested at a concentration of 25 µg/mL, the same hybrids demonstrated the highest DPPH antioxidant activity, with inhibition percentages of 84.1 and 83.2%, respectively, when compared to ascorbic acid (inhibition percentage of 89.5%).

摘要

在目前的研究中，通过水杨醛衍生物、氨基硫脲和 α-溴酮的反应制备了新的吗啉连接的噻唑。为了介导之前的三组分反应，使用两个当量进行反应。哌嗪在二恶烷中回流 5 小时。使用先前的协议，两个系列的噻唑，与芳烃或色烯单元相连，以良好到极好的收率制备。新的噻唑在 50 µM 的浓度下被检测为潜在的乙酰胆碱酯酶抑制剂。与多奈哌齐相比（抑制率为 92.8%），杂种11b和11c与 6-氯或 6-溴色烯-3-基单元相连，分别给出了 72.3% 和 71.5% 的最佳抑制百分比。此外，当以 25 µg/mL 的浓度进行测试时，与抗坏血酸（抑制百分比为 89.5%）相比，相同的杂交体表现出最高的 DPPH 抗氧化活性，抑制百分比分别为 84.1% 和 83.2%。