Low-toxicity amphiphilic molecules linked by an aromatic nucleus show broad-spectrum antibacterial activity and low drug resistance

被引：36
作者：
Chu, Wenchao [1 ]
Yang, Yi [1 ]
Qin, Shangshang [1 ,3 ]
Cai, Jianfeng [2 ]
Bai, Mengmeng [1 ]
Kong, Hongtao [1 ]
Zhang, En [1 ,3 ]
机构：
[1] Zhengzhou Univ, Minist Educ China, Key Lab Adv Pharmaceut Technol, Sch Pharmaceut Sci,Inst Drug Discovery & Dev, Zhengzhou 450001, Henan, Peoples R China
[2] Univ S Florida, Dept Chem, 4202 E Fowler Ave, Tampa, FL 33620 USA
[3] Collaborat Innovat Ctr New Drug Res & Safety Eval, Zhengzhou 450001, Henan, Peoples R China
来源：
CHEMICAL COMMUNICATIONS | 2019年 / 55卷 / 30期
基金：
中国博士后科学基金; 中国国家自然科学基金;
关键词：
DERIVATIVES; PEPTIDES;
D O I：
10.1039/c9cc00857h
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Amphiphilic molecules linked by an aromatic nucleus were developed that showed high selectivity toward bacteria over mammalian cells, and low drug resistance. A promising compound 4g exhibited strong bactericidal activity against a panel of sensitive and resistant bacteria, low toxicity, the ability to reduce cell viability in biofilms, stability in mammalian fluids, rapid killing of pathogens, and high in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA).<bold> </bold>
引用
收藏
页码：4307 / 4310
页数：4
相关论文
共 24 条
  • [1] A labelled-ubiquicidin antimicrobial peptide for immediate in situ optical detection of live bacteria in human alveolar lung tissue
    Akram, Ahsan R.
    Avlonitis, Nicolaos
    Lilienkampf, Annamaria
    Perez-Lopez, Ana M.
    McDonald, Neil
    Chankeshwara, Sunay V.
    Scholefield, Emma
    Haslett, Christopher
    Bradley, Mark
    Dhaliwal, Kevin
    [J]. CHEMICAL SCIENCE, 2015, 6 (12) : 6971 - 6979
  • [2] Ester- and amide-containing multiQACs: Exploring multicationic soft antimicrobial agents
    Allen, Ryan A.
    Jennings, Megan C.
    Mitchell, Myles A.
    Al-Khalifa, Saleh E.
    Wuest, William M.
    Minbiole, Kevin P. C.
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 27 (10) : 2107 - 2112
  • [3] Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles
    Bai, Peng-Yan
    Qin, Shang-Shang
    Chu, Wen-Chao
    Yang, Yi
    Cui, De-Yun
    Hua, Yong-Gang
    Yang, Qian-Qian
    Zhang, En
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2018, 155 : 925 - 945
  • [4] A re-evaluation of the role of host defence peptides in mammalian immunity
    Bowdish, DME
    Davidson, DJ
    Hancock, REW
    [J]. CURRENT PROTEIN & PEPTIDE SCIENCE, 2005, 6 (01) : 35 - 51
  • [5] Tackling antibiotic resistance
    Bush, Karen
    Courvalin, Patrice
    Dantas, Gautam
    Davies, Julian
    Eisenstein, Barry
    Huovinen, Pentti
    Jacoby, George A.
    Kishony, Roy
    Kreiswirth, Barry N.
    Kutter, Elizabeth
    Lerner, Stephen A.
    Levy, Stuart
    Lewis, Kim
    Lomovskaya, Olga
    Miller, Jeffrey H.
    Mobashery, Shahriar
    Piddock, Laura J. V.
    Projan, Steven
    Thomas, Christopher M.
    Tomasz, Alexander
    Tulkens, Paul M.
    Walsh, Timothy R.
    Watson, James D.
    Witkowski, Jan
    Witte, Wolfgang
    Wright, Gerry
    Yeh, Pamela
    Zgurskaya, Helen I.
    [J]. NATURE REVIEWS MICROBIOLOGY, 2011, 9 (12) : 894 - 896
  • [6] Synthesis and antibacterial evaluation of novel cationic chalcone derivatives possessing broad spectrum antibacterial activity
    Chu, Wen-Chao
    Bai, Peng-Yan
    Yang, Zhao-Qing
    Cui, De-Yun
    Hua, Yong-Gang
    Yang, Yi
    Yang, Qian-Qian
    Zhang, En
    Qin, Shangshang
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2018, 143 : 905 - 921
  • [7] Bacterial biofilms: A common cause of persistent infections
    Costerton, JW
    Stewart, PS
    Greenberg, EP
    [J]. SCIENCE, 1999, 284 (5418) : 1318 - 1322
  • [8] The 10 x '20 Initiative: Pursuing a Global Commitment to Develop 10 New Antibacterial Drugs by 2020
    Gilbert, David N.
    Guidos, Robert J.
    Boucher, Helen W.
    Talbot, George H.
    Spellberg, Brad
    Edwards, John E., Jr.
    Scheld, W. Michael
    Bradley, John S.
    Bartlett, John G.
    [J]. CLINICAL INFECTIOUS DISEASES, 2010, 50 (08) : 1081 - 1083
  • [9] Increased mortality associated with meticillin-resistant Staphylococcus aureus (MRSA) infection in the Intensive Care Unit: results from the EPIC II study
    Hanberger, Hakan
    Walther, Sten
    Leone, Marc
    Barie, Philip S.
    Rello, Jordi
    Lipman, Jeffrey
    Marshall, John C.
    Anzueto, Antonio
    Sakr, Yasser
    Pickkers, Peter
    Felleiter, Peter
    Engoren, Milo
    Vincent, Jean-Louis
    [J]. INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS, 2011, 38 (04) : 331 - 335
  • [10] Antibacterial and Antibiofilm Activity of Cationic Small Molecules with Spatial Positioning of Hydrophobicity: An in Vitro and in Vivo Evaluation
    Hoque, Jiaul
    Konai, Mohini M.
    Sequeira, Shanola S.
    Samaddar, Sandip
    Haldar, Jayanta
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2016, 59 (23) : 10750 - 10762
123