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新型磺酰基吡咯烷衍生物作为基质金属蛋白酶抑制剂的设计、合成与评价

Design, synthesis and evaluation of novel sulfonyl pyrrolidine derivatives as matrix metalloproteinase inhibitors.

作者信息

Cheng Xian-Chao, Wang Qiang, Fang Hao, Tang Wei, Xu Wen-Fang

机构信息

Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, No. 44 Wenhuaxi Road, Jinan 250012, China.

出版信息

Bioorg Med Chem. 2008 May 15;16(10):5398-404. doi: 10.1016/j.bmc.2008.04.027. Epub 2008 Apr 15.

DOI:10.1016/j.bmc.2008.04.027
PMID:18440232
Abstract

A series of novel sulfonyl pyrrolidine derivatives were designed, synthesized and assayed for their inhibitory activities on matrix metalloproteinase 2 (MMP-2) and aminopeptidase N (AP-N). The results showed that these pyrrolidine derivatives exhibited highly selective inhibition against MMP-2 as compared with AP-N. Compounds 6a-d were more potent MMP-2 inhibitors than the positive control LY52. The structure-activity relationships were also briefly discussed.

摘要

设计、合成了一系列新型磺酰基吡咯烷衍生物，并测定了它们对基质金属蛋白酶2（MMP-2）和氨肽酶N（AP-N）的抑制活性。结果表明，与AP-N相比，这些吡咯烷衍生物对MMP-2表现出高度选择性抑制作用。化合物6a-d作为MMP-2抑制剂比阳性对照LY52更有效。还简要讨论了构效关系。

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