Abstract
A series of 1beta-methyl-2-(naphthosultamyl)methyl-carbapenems bearing dicationic groups on the naphthosultamyl moiety was prepared and evaluated for activity against resistant gram-positive bacteria. Based on a combination of excellent in vitro antibacterial activity, acceptable mouse acute toxicity, and a desirable fragmentation pattern on beta-lactam ring opening, the analog 2g (L-786,392) was selected for extended evaluation.
MeSH terms
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Animals
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Carbapenems / chemical synthesis*
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Carbapenems / chemistry
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Carbapenems / pharmacology
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Carbapenems / toxicity
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Drug Resistance, Microbial
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Gram-Positive Bacteria / drug effects*
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Humans
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Lactams / chemistry
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Lactams / pharmacokinetics
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Lactams / pharmacology*
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Mice
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Microbial Sensitivity Tests
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Structure-Activity Relationship
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Thiazoles / chemistry
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Thiazoles / pharmacokinetics
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Thiazoles / pharmacology*
Substances
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Carbapenems
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Lactams
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Thiazoles
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L 786392