Abstract
The synthesis and biological evaluation of D-forphenicinol-cephalosporins are described. 7-Amino-3-(substituted)-3-cephem-4-carboxylic acid esters were coupled with N-tert-butoxy-carbonyl-D-forphenicinol derivatives. Most of cephalosporin analogs in this series had good antibacterial activities and were well absorbed from the gastrointestinal tract in mice. Among them, 7-(mono-O-methyl-D-forphenicinol)-3-propenyl analog showed the most significant result in biological evaluations.
MeSH terms
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Administration, Oral
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Animals
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Anti-Bacterial Agents / administration & dosage
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / pharmacokinetics*
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Anti-Bacterial Agents / pharmacology
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Bacteria / drug effects
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Cephalosporins / administration & dosage
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Cephalosporins / chemical synthesis
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Cephalosporins / pharmacokinetics*
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Cephalosporins / pharmacology
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Chemical Phenomena
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Chemistry
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Glycine / administration & dosage
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Glycine / analogs & derivatives*
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Glycine / chemical synthesis
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Glycine / pharmacokinetics
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Glycine / pharmacology
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Intestinal Absorption
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Male
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Mice
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Molecular Structure
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Staphylococcal Infections / drug therapy
Substances
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Anti-Bacterial Agents
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Cephalosporins
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forphenicinol
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Glycine