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Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus
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1993
Year
Antimicrobial ChemotherapyPharmaceutical ChemistryDrug ResistanceMedicinal ChemistrySeveral New 1-Carba-1-dethiacephalosporinsUnique ActivityAntimicrobial ResistanceHealth SciencesMethicillin-resistant Staphylococcus AureusBiochemistryStructure-activity RelationshipAntibacterial AgentAntimicrobial PharmacokineticsAntimicrobial CompoundPharmacologyClinical MicrobiologyAntimicrobial SusceptibilityMicrobiologyMedicineDrug Discovery
The synthesis and antimicrobial activity of several new 1-carba-1-dethiacephalosporins is described. The discovery of unique activity of some of the analogues against methicillin-resistant Staphylococcus aureus led to the development of a structure-activity relationship designed to optimize this activity. The results of this investigation along with the pharmacokinetic characteristics of select compounds are described.