Design, synthesis and preliminary evaluation of novel pyrrolidine derivatives as matrix metalloproteinase inhibitors
Design, synthesis and preliminary evaluation of novel pyrrolidine derivatives as matrix metalloproteinase inhibitors
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新型基质金属蛋白酶抑制剂吡咯烷衍生物的设计、合成及初步评价
DOI：
10.1016/j.ejmech.2007.12.020
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发表时间：
2008-10-01
影响因子：
6.7
通讯作者：
Xu, Wen-Fang
中科院分区：
文献类型：
--
作者：
Cheng, Xian-Chao;Wang, Qiang;Xu, Wen-Fang
设计、合成了一系列新型吡咯烷衍生物，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具有高度选择性抑制作用。异羟肟酸盐8a-c是与阳性对照LY 52相同或更有效的MMP-2抑制剂。提出了最强的化合物8a与MMP-2的结合模式。并简要讨论了构效关系。(C)2008年，Elsevier Masson SAS。All rights reserved.
A series of novel 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. The hydroxamates 8a-c were equally or more potent MMP-2 inhibitors than the positive control LY52. The binding mode of the most potent compound 8a with MMP-2 was proposed. Structure-activity relationships were also briefly discussed. (C) 2008 Elsevier Masson SAS. All rights reserved.