Search results for " Oxazolidinones"

showing 4 items of 4 documents

New linezolid-like 1,2,4-oxadiazoles active against Gram-positive multiresistant pathogens

2013

The synthesis and the in vitro antibacterial activity of novel linezolid-like oxadiazoles are reported. Replacement of the linezolid morpholine C-ring with 1,2,4-oxadiazole results in an antibacterial activity against Staphylococcus aureus both methicillin-susceptible and methicillin-resistant comparable or even superior to that of linezolid. While acetamidomethyl or thioacetoamidomethyl moieties in the C(5) side-chain are required, fluorination of the phenyl B ring exhibits a slight effect on an antibacterial activity but its presence seems to reduce the compounds cytotoxicity. Molecular modeling performed using two different approaches - FLAP and Amber software - shows that in the binding…

Methicillin-Resistant Staphylococcus aureusModels MolecularCell viabilityStaphylococcus aureusMolecular modelCell SurvivalMicrobial Sensitivity TestsAntimicrobial activityCrystallography X-Raymedicine.disease_causeDrug designMicrobiologyStructure-Activity Relationshipchemistry.chemical_compoundoxadiazoles linezolid antibioticsCell Line TumorDrug Resistance Multiple BacterialMorpholineAcetamidesDrug DiscoverymedicineHumansMoietyStructure–activity relationshipOxazolidinonesPharmacologyOxadiazolesOxazolidinones; Linezolid; Drug designDose-Response Relationship DrugMolecular StructureChemistryOrganic ChemistryLinezolidSettore CHIM/06 - Chimica OrganicaHep G2 CellsGeneral Medicinebiochemical phenomena metabolism and nutritionbacterial infections and mycosesSettore CHIM/08 - Chimica FarmaceuticaMethicillin-resistant Staphylococcus aureusCombinatorial chemistryOxazolidinoneAnti-Bacterial AgentsStaphylococcus aureusMED/07 - MICROBIOLOGIA E MICROBIOLOGIA CLINICALinezolidAntimicrobial activity; Cell viability; Drug design; Oxazolidinones; Staphylococcus aureusAntibacterial activitySoftware
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Synthesis and biological evaluation of 1,4-oxadiazole analogues of Linezolid

2012

Oxadiazoles Linezolid Oxazolidinones antibacterialsSettore CHIM/06 - Chimica OrganicaSettore CHIM/08 - Chimica Farmaceutica
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Sintesi e valutazione biologica di 1,2,4-ossadiazoli analoghi del Linezolid

2011

Settore CHIM/06 - Chimica Organicaoxadiazoles Linezolid anti-microbials oxazolidinonesSettore CHIM/08 - Chimica Farmaceutica
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Recent development in fluorinated antibiotics

2019

This chapter presents the most recent results in the development of fluorinated antibioticsby taking into consideration modern challenges of multidrug-resistant pathogens. After a brief introduction on the direct and indirect effects of fluorine and fluorinated moieties in regulating biological activity, the chapter is developed in three main subsections discussing the two major classes of fluorinated antibiotics, fluoroquinolones and oxazolidinones, plus an overview of recent research on the antibiotic activity of fluorinated analogs of tetracyclines, peptidomimetics, triazoles, and nucleosides. Discussed aspects include: (1) Synthesis and challenges posed by the introduction of fluorinate…

medicine.drug_classChemistryPeptidomimeticAntibiotics Fluorinated heterocycles Multidrug resistance Oxazolidinones QuinolonesAntibioticsmedicineSettore CHIM/06 - Chimica OrganicaCombinatorial chemistry
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