2015
Structure–Activity Relationship for the Oxadiazole Class of Antibiotics
Spink E, Ding D, Peng Z, Boudreau M, Leemans E, Lastochkin E, Song W, Lichtenwalter K, O’Daniel P, Testero S, Pi H, Schroeder V, Wolter W, Antunes N, Suckow M, Vakulenko S, Chang M, Mobashery S. Structure–Activity Relationship for the Oxadiazole Class of Antibiotics. Journal Of Medicinal Chemistry 2015, 58: 1380-1389. PMID: 25590813, PMCID: PMC6863074, DOI: 10.1021/jm501661f.Peer-Reviewed Original ResearchConceptsMethicillin-resistant S. aureusStructure-activity relationshipsOxadiazole classClasses of antibioticsLinezolid-resistant S. aureusS. aureusMRSA infectionLead structuresCrystal structureMouse modelIndol-5Lower clearanceExhibit activityAntibioticsSilico dockingBacterium Staphylococcus aureusStaphylococcus aureusInfectionGram-positive bacterium Staphylococcus aureusCell wall biosynthesisPenicillin-binding proteinsGreat promiseAureus
2014
Discovery of a New Class of Non-β-lactam Inhibitors of Penicillin-Binding Proteins with Gram-Positive Antibacterial Activity
O’Daniel P, Peng Z, Pi H, Testero S, Ding D, Spink E, Leemans E, Boudreau M, Yamaguchi T, Schroeder V, Wolter W, Llarrull L, Song W, Lastochkin E, Kumarasiri M, Antunes N, Espahbodi M, Lichtenwalter K, Suckow M, Vakulenko S, Mobashery S, Chang M. Discovery of a New Class of Non-β-lactam Inhibitors of Penicillin-Binding Proteins with Gram-Positive Antibacterial Activity. Journal Of The American Chemical Society 2014, 136: 3664-3672. PMID: 24517363, PMCID: PMC3985699, DOI: 10.1021/ja500053x.Peer-Reviewed Original ResearchConceptsMethicillin-resistant Staphylococcus aureusPenicillin-binding protein 2aLinezolid-resistant methicillin-resistant Staphylococcus aureusNon-β-lactam antibioticsGlobal public health concernSerious global public health concernPublic health concernClasses of antibioticsMouse modelVivo efficacyOral bioavailabilityProtein 2ABactericidal activityGram-positive antibacterial activityStaphylococcus aureusNon-β-lactam inhibitorsInfectionPenicillin binding proteinsAntibioticsAntibacterial activityVancomycin