Synthesis and biological evaluation of novel fused indolo [3, 2-c] [1,8] naphthyridine derivatives as potential antibacterial agents

被引:8
|
作者
Makhanya, Talent Raymond [1 ]
Gengan, Robert Moonsamy [1 ]
Ata, Athar [2 ]
机构
[1] Durban Univ Technol, Fac Sci Appl, Dept Chem, POB 1334,Steve Biko Campus, ZA-4001 Durban, South Africa
[2] Univ Winnipeg, Richardson Coll Environm Sci Complex, Dept Chem, Winnipeg, MB, Canada
基金
新加坡国家研究基金会;
关键词
Antibacterial activity; indolo-naphthyridine; mutagenicity; Povarov reaction; POVAROV REACTION-SYNTHESIS; QUINOLINES; INHIBITORS;
D O I
10.1080/00397911.2019.1573373
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Nine novel fused indolo [1,8] naphthyridine derivatives were synthesized using the Povarov reaction, in a one-pot system, and were fully characterized by spectroscopic techniques such as FT-IR, NMR, TOF-MS, and elemental analysis. Furthermore, their antibacterial activities against six bacterial strains were assessed. The results of the bioassay demonstrated that compounds 4a, 4c, and 4i showed good inhibitory effect with a MIC value ranging from 0.04687 to 0.09375 mu M against Bacillus cereus and Staphylococcus aureus. The toxicity of 4a-i, evaluated through mutagenicity test against Salmonella typhimurium TA 98 and TA100 strains, revealed that there was no significant increase in the number of revertant colonies in comparison with the control, sodium azide. [GRAPHICS] .
引用
收藏
页码:823 / 835
页数:13
相关论文
共 50 条
  • [21] Design, Synthesis, and In Vitro Evaluation of Benzofuro[3,2-c]Quinoline Derivatives as Potential Antileukemia Agents
    Lin, Ying
    Xing, Dong
    Wu, Wen-Biao
    Xu, Gao-Ya
    Yu, Li-Fang
    Tang, Jie
    Zhou, Yu-Bo
    Li, Jia
    Yang, Fan
    MOLECULES, 2020, 25 (01):
  • [22] Synthesis and evaluation of novel urea and amide derivatives of 2-amino-4-phenylthiazole as potential antibacterial agents
    Zhang, Zhi-Hua
    Chen, Yu
    Yan, Xin-Jia
    Sun, Yao
    Yang, Xiao-Man
    Cai, Xiao-Yu
    You, Song
    MEDICINAL CHEMISTRY RESEARCH, 2017, 26 (09) : 2080 - 2087
  • [23] Synthesis and biological evaluation of novel benzoxazinyl-oxazolidinones as potential antibacterial agents
    Guo, Bin
    Fan, Houxing
    Xin, Qisheng
    Chu, Wenjing
    Wang, Hui
    Yang, Yushe
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2013, 23 (13) : 3697 - 3699
  • [24] Synthesis and biological evaluation of coumarin derivatives containing imidazole skeleton as potential antibacterial agents
    Hu, Yang
    Shen, Yufeng
    Wu, Xiaohu
    Tu, Xiao
    Wang, Gao-Xue
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2018, 143 : 958 - 969
  • [25] Synthesis and Biological Evaluation of Novel Phenothiazine-Sulfonamide Based Isoxazole Derivatives as Potent Antibacterial Agents
    Mallam, Vasudha
    Kumar, M. Ranadheer
    Vijayakumar, Baru
    RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY, 2022, 48 (03) : 596 - 600
  • [26] Design, synthesis and biological evaluation of novel indole-piperazine derivatives as antibacterial agents
    Liu, Ting
    Yao, Xiaofang
    Zhang, Rongrong
    Wu, Tianling
    Liu, Zhigang
    Li, Ding
    Dong, Qingjian
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2023, 89
  • [27] Synthesis and biological evaluation of novel ocotillol-type triterpenoid derivatives as antibacterial agents
    Zhou, Zhiwen
    Ma, Cong
    Zhang, Hengyuan
    Bi, Yi
    Chen, Xia
    Tian, Hua
    Xie, Xiaoni
    Meng, Qingguo
    Lewis, Peter John
    Xu, Jinyi
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2013, 68 : 444 - 453
  • [28] Novel pleuromutilin derivatives as antibacterial agents: Synthesis, biological evaluation and molecular docking studies
    Wang, Xinyang
    Ling, Yong
    Wang, Hui
    Yu, Jianghe
    Tang, Junming
    Zheng, Heng
    Zhao, Xi
    Wang, Donggeng
    Chen, Guangtong
    Qiu, Wenqian
    Tao, Jinhua
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2012, 22 (19) : 6166 - 6172
  • [29] Synthesis and Biological Evaluation of Some Novel Fused Pyrazolopyrimidines as Potential Anticancer and Antimicrobial Agents
    Abd El Razik, Heba A.
    Wahab, Abeer E. Abdel
    ARCHIV DER PHARMAZIE, 2011, 344 (03) : 184 - 196
  • [30] Synthesis and biological evaluation of novel 2-alkoxycarbonylallylester phosphonium derivatives as potential anticancer agents
    Gardner, Zachary S.
    Schumacher, Tanner J.
    Ronayne, Conor T.
    Kumpati, Greeshma P.
    Williams, Michael J.
    Yoshimura, Akira
    Palle, Hithardha
    Mani, Chinnadurai
    Rumbley, Jon
    Mereddy, Venkatram R.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021, 45