Abstract
Penicillin sulfones, which structurally incorporate both a 6-position alkylidene substituent and a 2'beta substituent, have been synthesized and evaluated as inhibitors of class C and class A serine beta-lactamases. Incorporation of the 2'beta-substituent generally improves inhibitory activity. Substituents that improve transport across the bacterial cell membrane have also been incorporated.
MeSH terms
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Cloxacillin / analogs & derivatives*
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Cloxacillin / chemical synthesis*
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Cloxacillin / chemistry*
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Cloxacillin / pharmacology
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Drug Therapy, Combination / pharmacology
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacology*
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Inhibitory Concentration 50
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Microbial Sensitivity Tests
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Penicillin Resistance
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Piperacillin / pharmacology
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Structure-Activity Relationship
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Sulfones / chemistry
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beta-Lactamase Inhibitors*
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beta-Lactamases
Substances
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Enzyme Inhibitors
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Sulfones
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beta-Lactamase Inhibitors
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beta-Lactamases
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beta-lactamase TEM-1
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Cloxacillin
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Piperacillin