丙氨酸酯衍生物的合成及其对吲哚美辛的经皮促渗活性

摘要

Seven novel 2-(N,N-diethylamino)propanoates (1a~1g) were synthesized using N,N-di-ethyl-l-alanine as material, N,N-dicyclohexylcarbodiimide as condensation agent and 4-dimethylamin-opyridine as catalyst. The structures were characterized by 1 H NMR, MS( ESI) and elemental analy-sis. In vitro penetration enhancing activities of 1 were evaluated using rat skins as biomembrane and in-domethacin as model drug in TT-18-type diffusion cells. The results showed that 1 g exhibited good skin penetration enhancement of indomethacin(94. 2%).%以N,N-二乙基-l-丙氨酸为原料,N,N′-二环己基碳二亚胺为缩合剂,4-甲氨基吡啶为催化剂,合成了7个新型的2-(N,N′-二乙基氨基)丙酸酯(1a~1g),其结构经1H NMR, MS(ESI)和元素分析表征。研究了其对药物吲哚美辛的体外经皮促渗活性。结果表明：1g对吲哚美辛的经皮促渗活性最好(94.2%)。