Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Sequence
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CD13 Antigens / antagonists & inhibitors
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CD13 Antigens / chemistry
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Drug Design*
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Matrix Metalloproteinase 2 / chemistry
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Matrix Metalloproteinase Inhibitors*
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Matrix Metalloproteinases / chemistry
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Models, Molecular
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Molecular Conformation
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Pyrrolidines / chemical synthesis*
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Pyrrolidines / chemistry
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Pyrrolidines / pharmacology*
Substances
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Enzyme Inhibitors
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Matrix Metalloproteinase Inhibitors
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Pyrrolidines
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CD13 Antigens
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Matrix Metalloproteinases
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Matrix Metalloproteinase 2
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pyrrolidine