The oxadiazole antibacterials

被引:39
作者
Janardhanan, Jeshina [1 ]
Chang, Mayland [1 ]
Mobashery, Shahriar [1 ]
机构
[1] Univ Notre Dame, Dept Chem & Biochem, Notre Dame, IN 46556 USA
基金
美国国家卫生研究院;
关键词
RESISTANT STAPHYLOCOCCUS-AUREUS; PENICILLIN-BINDING PROTEINS; AIDED DRUG DISCOVERY; CELL-WALL; ANTIBIOTICS; METABOLISM; PATHOGENS; ESKAPE; MMPL;
D O I
10.1016/j.mib.2016.05.009
中图分类号
Q93 [微生物学];
学科分类号
071005 ; 100705 ;
摘要
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.
引用
收藏
页码:13 / 17
页数:5
相关论文
共 29 条
  • [1] Epidemiology of methicillin-resistant Staphylococcus aureus
    Boucher, Helen W.
    Corey, G. Ralph
    [J]. CLINICAL INFECTIOUS DISEASES, 2008, 46 : S344 - S349
  • [2] CDC, 2013, ANT RES THREATS US
  • [3] A Historical Overview of Natural Products in Drug Discovery
    Dias, Daniel A.
    Urban, Sylvia
    Roessner, Ute
    [J]. METABOLITES, 2012, 2 (02) : 303 - 336
  • [4] Exploration of the structure-activity relationship of 1,2,4-oxadiazole antibiotics
    Ding, Derong
    Boudreau, Marc A.
    Leemans, Erika
    Spink, Edward
    Yamaguchi, Takao
    Testero, Sebastian A.
    O'Daniel, Peter I.
    Lastochkin, Elena
    Chang, Mayland
    Mobashery, Shahriar
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2015, 25 (21) : 4854 - 4857
  • [5] How to cope with the quest for new antibiotics
    Fabbretti, Attilio
    Gualerzi, Claudio O.
    Brandi, Letizia
    [J]. FEBS LETTERS, 2011, 585 (11) : 1673 - 1681
  • [6] Frimodt-Moller N., 1999, Handbook of animal model of infection, P127, DOI DOI 10.1016/B978-012775390-4/50153-6
  • [7] β-Lactam resistance in Staphylococcus aureus: the adaptive resistance of a plastic genome
    Fuda, CCS
    Fisher, JF
    Mobashery, S
    [J]. CELLULAR AND MOLECULAR LIFE SCIENCES, 2005, 62 (22) : 2617 - 2633
  • [8] PENICILLIN-BINDING PROTEINS AND BACTERIAL-RESISTANCE TO BETA-LACTAMS
    GEORGOPAPADAKOU, NH
    [J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1993, 37 (10) : 2045 - 2053
  • [9] The re-emergence of natural products for drug discovery in the genomics era
    Harvey, Alan L.
    Edrada-Ebel, RuAngelie
    Quinn, Ronald J.
    [J]. NATURE REVIEWS DRUG DISCOVERY, 2015, 14 (02) : 111 - 129
  • [10] The emergence and evolution of methicillin-resistant Staphylococcus aureus
    Hiramatsu, K
    Cui, L
    Kuroda, M
    Ito, T
    [J]. TRENDS IN MICROBIOLOGY, 2001, 9 (10) : 486 - 493