title: The oxadiazole antibacterials.
abstract: The oxadiazoles are a class of antibacterials discovered by in silico docking and scoring of compounds against the X-ray structure of a penicillin-binding protein. These antibacterials exhibit activity against Gram-positive bacteria, including against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE). They show in vivo efficacy in murine models of peritonitis/sepsis and neutropenic thigh MRSA infection. They are bactericidal and orally bioavailable. The oxadiazoles show promise in treatment of MRSA infection.
authors.affiliation: Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, United States.
authors.forename: Jeshina
authors.initials: J
authors.lastname: Janardhanan
authors.affiliation: Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, United States. Electronic address: mchang@nd.edu.
authors.forename: Mayland
authors.initials: M
authors.lastname: Chang
authors.affiliation: Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, United States. Electronic address: mobashery@nd.edu.
authors.forename: Shahriar
authors.initials: S
authors.lastname: Mobashery
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000627:therapeutic use*; D005260:Female; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D051379:Mice; D008813:Mice, Inbred ICR; D008826:Microbial Sensitivity Tests; D010069:Oxadiazoles / Q000627:therapeutic use*; D010538:Peritonitis / Q000188:drug therapy / Q000382:microbiology; D021281:Quantitative Structure-Activity Relationship; D013203:Staphylococcal Infections / Q000188:drug therapy* / Q000382:microbiology; D065507:Vancomycin-Resistant Enterococci / Q000187:drug effects*; D047090:beta-Lactams / Q000627:therapeutic use*
chemical_list: D000900:Anti-Bacterial Agents; D010069:Oxadiazoles; D047090:beta-Lactams