Small Scorpion-like Peptidomimetics: Potential Broad-Spectrum Membrane Active Antimicrobials without Detectable Resistance

被引：2
|
作者：
Zhang, En [1 ]
Qin, Shangshang [1 ]
机构：
[1] Zhengzhou Univ, Sch Pharmaceut Sci, Inst Drug Discovery & Dev, Key Lab Adv Pharmaceut Technol,Minist Educ, Zhengzhou 450001, Peoples R China
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2021年 / 64卷 / 14期
关键词：
D O I：
10.1021/acs.jmedchem.1c01065
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Peptidomimetics have been explored as potential antimicrobial agents against Gram-positive and Gram-negative bacteria. A new scorpion-like peptidomimetic, compound 12, inspired by molecular design in bioengineering, exhibited excellent antimicrobial activity and good selectivity between bacteria and human cells. In addition, compound 12 showed impressive therapeutic efficacy with 99.998% reduction in the in vivo model.
引用
收藏
页码：9891 / 9893
页数：3
相关论文
共 5 条
  • [1] Membrane Active Small Molecules Show Selective Broad Spectrum Antibacterial Activity with No Detectable Resistance and Eradicate Biofilms
    Hoque, Jiaul
    Konai, Mohini M.
    Gonuguntla, Spandhana
    Manjunath, Goutham B.
    Samaddar, Sandip
    Yarlagadda, Venkateswarlu
    Haldar, Jayanta
    JOURNAL OF MEDICINAL CHEMISTRY, 2015, 58 (14) : 5486 - 5500
  • [2] Unique iminotetrahydroberberine-corbelled metronidazoles as potential membrane active broad-spectrum antibacterial agents
    Ansari, Mohammad
    Tan, Yi-Min
    Sun, Hang
    Li, Shuo
    Zhou, Cheng-He
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2022, 76
  • [3] Design of phenothiazine-based cationic amphiphilic derivatives incorporating arginine residues: Potential membrane-active broad-spectrum antimicrobials combating pathogenic bacteria in vitro and in vivo
    Yu, Qian
    Cai, Qiongna
    Liang, Wanxin
    Zhong, Kewen
    Liu, Jiayong
    Li, Haizhou
    Chen, Yongzhi
    Li, Hongxia
    Fang, Shanfang
    Zhong, Rongcui
    Liu, Shouping
    Lin, Shuimu
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023, 260
  • [4] Tomato receptor-like cytosolic kinase RIPK confers broad-spectrum disease resistance without yield penalties
    Wang, Ran
    Li, Chenying
    Li, Qinghong
    Ai, Yingfei
    Huang, Zeming
    Sun, Xun
    Zhou, Jie
    Zhou, Yanhong
    Liang, Yan
    HORTICULTURE RESEARCH, 2022, 9
  • [5] Membrane-Active All-Hydrocarbon-Stapled α-Helical Amphiphilic Tat Peptides: Broad-Spectrum Antibacterial Activity and Low Incidence of Drug Resistance
    Li, Shu
    Wang, Zhaopeng
    Song, Shibo
    Tang, Yuanyuan
    Zhou, Jingjing
    Liu, Xiaojing
    Zhang, Xingjiao
    Chang, Min
    Wang, Kairong
    Peng, Yali
    ACS INFECTIOUS DISEASES, 2024, 10 (05): : 1839 - 1855
1