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Design, synthesis and biological activity evaluation of benzoate compounds as local anesthetics

机译：苯甲酸酯化合物作为局部麻醉剂的设计，合成及生物活性评价

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Tetracaine and pramocaine were used as the lead compounds to design benzoate compounds. The combination principle was used to design the target molecule, and the target molecule was modified by bioisostere formation and modification with alkyl groups. In this research, a total of 16 compounds were designed and synthesized. In the process of synthesis, we selected a route with high total yields, mild conditions and simple operation. Three steps were used in the synthesis of the new target compounds, namely, alkylation, esterification and alkylation. The newly designed target compounds were evaluated via surface anesthesia, infiltration anesthesia, block anesthesia and acute toxicity tests. The results of biological activity experiments showed that compounds 4d , 4g , 4j , 4k , 4n , and 4o had a good local anesthetic effect, and the results of acute toxicity tests showed that the target compounds had low toxicity.
机译：用硫妥和普拉克因作为铅化合物以设计苯甲酸酯化合物。使用组合原理来设计靶分子，并通过Bioisostere的形成和用烷基改性来改变靶分子。在该研究中，共设计并合成了总共16种化合物。在合成过程中，我们选择了高总产量，温和条件和操作简单的途径。在新靶化合物的合成中使用三个步骤，即烷基化，酯化和烷基化。通过表面麻醉，浸润麻醉，阻断麻醉和急性毒性测试评估新设计的目标化合物。生物活性实验的结果表明，化合物4d，4g，4j，4k，4n和4o具有良好的局部麻醉效果，并且急性毒性试验结果表明，靶化合物的毒性低。

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