Abstract
The synthesis of a new series of 6-acylamino penam derivatives and their inhibition of cysteine proteases cathepsins B, L, K, and S is described. The 6-acylamino-penam sulfone compounds showed excellent cathepsin L, K, and S inhibition activity with IC(50) values in the nanomolar and subnanomolar range.
MeSH terms
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Amines / chemistry*
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Cathepsins / antagonists & inhibitors*
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Cysteine Proteinase Inhibitors / chemical synthesis*
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Cysteine Proteinase Inhibitors / pharmacology*
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Inhibitory Concentration 50
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Lactams / chemistry*
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Lactams / pharmacology*
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Structure-Activity Relationship
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Sulfones / chemistry*
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Sulfones / pharmacology*
Substances
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Amines
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Cysteine Proteinase Inhibitors
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Lactams
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Sulfones
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4-oxa-1-azabicyclo(3.2.0)heptan-7-one
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Cathepsins