The oxadiazole antibacterials

被引：40

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

来源：

CURRENT OPINION IN MICROBIOLOGY | 2016年 / 33卷

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

页码：13 / 17

页数：5

共 29 条

[1] Epidemiology of methicillin-resistant Staphylococcus aureus [J].

Boucher, Helen W. ;

Corey, G. Ralph .

CLINICAL INFECTIOUS DISEASES, 2008, 46 :S344-S349

[2]

CDC, 2013, ANT RES THREATS US

[3] A Historical Overview of Natural Products in Drug Discovery [J].

Dias, Daniel A. ;

Urban, Sylvia ;

Roessner, Ute .

METABOLITES, 2012, 2 (02) :303-336

[4] Exploration of the structure-activity relationship of 1,2,4-oxadiazole antibiotics [J].

Ding, Derong ;

Boudreau, Marc A. ;

Leemans, Erika ;

Spink, Edward ;

Yamaguchi, Takao ;

Testero, Sebastian A. ;

O'Daniel, Peter I. ;

Lastochkin, Elena ;

Chang, Mayland ;

Mobashery, Shahriar .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2015, 25 (21) :4854-4857

[5] How to cope with the quest for new antibiotics [J].

Fabbretti, Attilio ;

Gualerzi, Claudio O. ;

Brandi, Letizia .

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 [J].

Fuda, CCS ;

Fisher, JF ;

Mobashery, S .

CELLULAR AND MOLECULAR LIFE SCIENCES, 2005, 62 (22) :2617-2633

[8] PENICILLIN-BINDING PROTEINS AND BACTERIAL-RESISTANCE TO BETA-LACTAMS [J].

GEORGOPAPADAKOU, NH .

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1993, 37 (10) :2045-2053

[9] The re-emergence of natural products for drug discovery in the genomics era [J].

Harvey, Alan L. ;

Edrada-Ebel, RuAngelie ;

Quinn, Ronald J. .

NATURE REVIEWS DRUG DISCOVERY, 2015, 14 (02) :111-129

[10] The emergence and evolution of methicillin-resistant Staphylococcus aureus [J].

Hiramatsu, K ;

Cui, L ;

Kuroda, M ;

Ito, T .

TRENDS IN MICROBIOLOGY, 2001, 9 (10) :486-493

← 1 2 3 →