2-乙酰氧基-3-苯基-4-α-羟苄基-N-甲基-γ-内酰胺的合成及活性评价

Synthesis and Activity Evaluation of 2-Acetoxy-3-phenyl-4-α-methylol-N-methyl-γ-lactam

以2-羟基-3-苯基-4-苯甲酰基-N-甲基-γ-内酰胺(■)为原料,通过酰化、还原反应合成化合物2-乙酰氧基-3-苯基-4-α-羟苄基-N-甲基-γ-内酰胺(■),两步反应总收率为63.13%。■对乙酰胆碱酯酶的抑制活性、谷丙转氨酶活性及黄疸指数的影响不明显。■的2位乙酰化对乙酰胆碱酯酶抑制作用和降低谷丙转氨酶作用不明显,对黄疸指数几乎无影响,进一步的结构修饰及活性评价正在进行中。

Title compound 3 Acetylation on the position 2 glutamic-pyruvic transaminase evaluation are in progress. was synthesized from of compound 1 has no （GPT） depression and compound 1 in two steps in a total yield of 63.13%. obvious effect on acetylcholinesterase inhibitory activity, icterus index. Further structural modification and activity