Abstract
Novel sulfonamide matrix metalloproteinase inhibitors of general formula (9) were synthesised by a route involving a stereoselective conjugate addition reaction. Enzyme selectivity was found to be dependant on the nature of the sulfonamide substituents. Compounds (9f, 9q) are potent selective collagenase inhibitors with good oral bioavailability.
MeSH terms
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Administration, Oral
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Animals
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology
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Biological Availability
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Hydrogen Bonding
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Hydroxamic Acids / chemistry
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Hydroxamic Acids / pharmacology
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Matrix Metalloproteinase Inhibitors*
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Molecular Structure
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Protease Inhibitors / chemical synthesis*
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Protease Inhibitors / pharmacology
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Rats
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Sulfonamides / chemical synthesis*
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Sulfonamides / pharmacology
Substances
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Antineoplastic Agents
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Hydroxamic Acids
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Matrix Metalloproteinase Inhibitors
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Protease Inhibitors
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Sulfonamides
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marimastat