新型强效 2,5-吡咯烷二酮类肽类似物作为氨基肽酶 N 的抑制剂。设计、合成与活性评价。
Novel potent 2,5-pyrrolidinedione peptidomimetics as aminopeptidase N inhibitors. Design, synthesis and activity evaluation.
机构信息
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Central South University, 172 Tongzipo Road, 410013 Changsha, Hu'nan, China.
出版信息
Bioorg Med Chem Lett. 2012 Jan 15;22(2):850-3. doi: 10.1016/j.bmcl.2011.12.048. Epub 2011 Dec 16.
A series of novel aminopeptidase N inhibitors with 2,5-pyrrolidinedione scaffold were chemically synthesized. Their preliminary biological activities in enzyme kinetics and cell assay in vitro and anti-metastasis profile in vivo were also evaluated. The results indicated that all the compounds displayed potent inhibitory activity against aminopeptidase N. Compound 8f inhibited aminopeptidase N activity with IC(50) value of 1.0μM and displayed better activity profile in vivo than that of bestatin.
一系列具有 2,5-吡咯烷二酮骨架的新型氨基肽酶 N 抑制剂被化学合成。它们在体外酶动力学和细胞测定以及体内抗转移谱中的初步生物学活性也得到了评估。结果表明，所有化合物均表现出对氨基肽酶 N 的强烈抑制活性。化合物 8f 对氨基肽酶 N 的抑制活性的 IC50 值为 1.0μM，其体内活性谱优于最佳替丁。
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