Gregán F, Novomeský P, Racanská E, Kettmann V
Departament of Organic Chemistry, Faculty of Pharmacy, Bratislava, Czechoslovakia.
Farmaco. 1992 Mar;47(3):327-34.
A series of 8 new derivatives of 2-alkoxyphenylcarbamoic acid were synthesized and assayed for local anesthetic activity. The above compounds were isolated as hydrochlorides and their structure was proved by 1H NMR, 13C NMR and IR spectroscopy. The index of anesthetic activity of the compounds in infiltration and surface anesthesia increases with the length of the alkyl chain and, except for the C1-C3 congeners, all higher homologues proved to be significantly more active than the standard reference compounds, procaine and cocaine, respectively. Toxicity of the drugs decreases with increasing the chain length and is within acceptable limits.
合成了一系列8种新的2-烷氧基苯基氨基甲酸衍生物，并对其局部麻醉活性进行了测定。上述化合物以盐酸盐形式分离出来，其结构通过1H NMR、13C NMR和红外光谱得以证实。这些化合物在浸润麻醉和表面麻醉中的麻醉活性指数随烷基链长度的增加而升高，除了C1 - C3同系物外，所有更高的同系物分别被证明比标准参考化合物普鲁卡因和可卡因活性显著更高。药物的毒性随链长增加而降低，且在可接受范围内。
