Synthesis of new sulfonyl pyrrolidine derivatives as matrix metalloproteinase inhibitors
Synthesis of new sulfonyl pyrrolidine derivatives as matrix metalloproteinase inhibitors
复制标题
新型磺酰吡咯烷衍生物作为基质金属蛋白酶抑制剂的合成
DOI：
10.1016/j.bmc.2008.07.073
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发表时间：
2008-09-01
影响因子：
3.5
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、合成了一系列新的磺酰基吡咯烷类化合物，并测定了它们对基质金属蛋白酶2(MMP2)和氨基肽酶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基质金属蛋白酶-2具有高度的选择性抑制作用。化合物4c、4j、5a和5b是与阳性对照LY52相同或更有效的基质金属蛋白酶-2抑制剂。Flexx对接是为了解释基质金属蛋白酶-2和AP-N活性不同的原因。对构效关系也作了简要讨论。(C)2008爱思唯尔有限公司。保留所有权利。
A series of new sulfonyl pyrrolidine derivatives was 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 compounds 4c, 4j, 5a, and 5b were equally or more potent MMP-2 inhibitors than the positive control LY52. The FlexX docking was done to explain the reason for the different potency between MMP-2 and AP-N. Structure-activity relationships were also briefly discussed. (C) 2008 Elsevier Ltd. All rights reserved.