Discovery of Antibiotic (E)‑3-(3-Carboxyphenyl)-2-(4-cyanostyryl)quinazolin-4(3H)‑one
Bouley R, Kumarasiri M, Peng Z, Otero L, Song W, Suckow M, Schroeder V, Wolter W, Lastochkin E, Antunes N, Pi H, Vakulenko S, Hermoso J, Chang M, Mobashery S. Discovery of Antibiotic (E)‑3-(3-Carboxyphenyl)-2-(4-cyanostyryl)quinazolin-4(3H)‑one. Journal Of The American Chemical Society 2015, 137: 1738-1741. PMID: 25629446, PMCID: PMC4607046, DOI: 10.1021/jacs.5b00056.Peer-Reviewed Original ResearchStructure–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