2015
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 ResearchConceptsChemical synthesisMethicillin-resistant Staphylococcus aureusSilico dockingDiscovery of antibioticsNovel classCell wall biosynthesisPenicillin-binding protein 2aMRSA infectionClasses of antibioticsClinical challengeQuinazolinones
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