Abstract
A series of succinyl hydroxamate MMP inhibitors were prepared incorporating an aryl amino ketone moiety in place of the more typical C-terminal amino acid amides. Compounds of the C-terminal ketone series displayed potent inhibition of MMPs. Several compounds of the series were shown to be orally bioavailable.
MeSH terms
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Gelatinases / antagonists & inhibitors*
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Hydroxamic Acids / pharmacology*
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Ketones / pharmacology*
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Matrix Metalloproteinase 1
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Matrix Metalloproteinase 2
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Matrix Metalloproteinase 7
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Matrix Metalloproteinase Inhibitors*
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Metalloendopeptidases / antagonists & inhibitors*
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Protease Inhibitors / pharmacology*
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Structure-Activity Relationship
Substances
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Hydroxamic Acids
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Ketones
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Matrix Metalloproteinase Inhibitors
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Protease Inhibitors
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Gelatinases
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Metalloendopeptidases
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Matrix Metalloproteinase 7
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Matrix Metalloproteinase 2
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Matrix Metalloproteinase 1