Journal of Medicinal Chemistry · 1993 · 10 citations · 0 references
PharmacyMedicinal ChemistryPharmacokineticsDrug DiscoveryDrug MetabolismStructure-activity RelationshipsAnaerobic BacteriologyAntibiotic ResistanceAntimicrobial PharmacodynamicsLead Compound DesignLead DiscoveryNatural Product Drug DiscoveryAnaerobic Infection TreatmentAnaerobic PathogenesisBiological Evaluation ReportGram-negative AnaerobesLead Compound OptimizationPharmacokinetic ParametersToxicological EvaluationToxicological Profile
The synthesis and biological evaluation of novel 1-carba-1-dethiacephalosporins exhibiting activity against anaerobic pathogens are described. The nitrothiazole substituent was determined to be crucial to maintaining this activity. The pharmacokinetic parameters and initial toxicological profile of the lead compound are discussed.