Abstract
Several classes of arylsulfone-based MMP-2/-9 inhibitors utilizing 6- to 8-membered heterocyclic rings as zinc-binding groups (ZBGs) have been synthesized and their enzyme inhibitory activities were evaluated. Although a number of 6- and 7-membered heterocycles were effective, the most potent arylsulfone inhibitors are based on the rigid 1- or 3-hydroxypyridone ZBG.
MeSH terms
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Heterocyclic Compounds / chemical synthesis*
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Heterocyclic Compounds / chemistry
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Heterocyclic Compounds / pharmacology*
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Lactams / chemical synthesis
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Lactams / chemistry
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Lactams / pharmacology
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Matrix Metalloproteinase Inhibitors*
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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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Pyridones / chemistry
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Pyridones / pharmacology
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Structure-Activity Relationship
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Sulfones / chemical synthesis*
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Sulfones / chemistry
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Sulfones / pharmacology*
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Zinc / chemistry*
Substances
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Heterocyclic Compounds
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Lactams
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Matrix Metalloproteinase Inhibitors
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Protease Inhibitors
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Pyridones
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Sulfones
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Zinc