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肽类化合物在胃肠道易被酶破坏,吸收也很差;注射给药时,肽类一旦进入血流,可因血浆与组织肽酶而引起水解代谢而导致半衰期缩短。故注射给药存在问题。将生物活性肽制成前体药物是解决药物释放及输送的一种有效方法。作者发现,4-咪唑酮在几乎所有肽的α-氨基酰胺结构部位是一种有效的前体药物。本文通过丙酮和不同的二肽类(丙氨酸-甘氨酸,丙氨酸-丙氨酸,苯丙氨酸-亮氨酸,亮氨酸-甘氨酸,门冬氨酸-苯丙氯酸甲基酯)缩合的5种4-咪唑酮水解动力学的研究,与对苯丙氨酸-亮氨酸衍生物及其母体二肽
Peptides in the gastrointestinal tract easily damaged by enzymes, absorption is also poor; injection, once the peptide into the blood stream, due to plasma and tissue peptidase caused by hydrolysis and metabolism resulting in shortened half-life. So there is a problem with injection. Preparing bioactive peptides as prodrugs is an effective way to solve the problem of drug release and delivery. The authors found that 4-imidazolidinone is a potent prodrug at the α-aminoamide moiety of almost all peptides. In this paper, the effects of different concentrations of acetone and different dipeptides (alanine-glycine, alanine-alanine, phenylalanine-leucine, leucine-glycine, aspartic acid- Ester) condensation of five kinds of 4-imidazolone hydrolysis kinetics of the study, and p-phenylalanine-leucine derivatives and their parent dipeptide