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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Binding Sites / drug effects
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CD13 Antigens / antagonists & inhibitors
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Computer Simulation
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Crystallography, X-Ray
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Drug Design*
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Drug Evaluation, Preclinical
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Matrix Metalloproteinase Inhibitors*
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Models, Molecular
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Molecular Conformation
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Protease Inhibitors / chemical synthesis
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Protease Inhibitors / chemistry
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Protease Inhibitors / pharmacology*
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Pyrrolidines / chemical synthesis
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Pyrrolidines / chemistry
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Pyrrolidines / pharmacology*
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Stereoisomerism
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Structure-Activity Relationship
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Sulfones / chemistry*
Substances
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Matrix Metalloproteinase Inhibitors
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Protease Inhibitors
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Pyrrolidines
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Sulfones
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CD13 Antigens