Original Article | Published:

Synthesis and biological evaluation of indole core-based derivatives with potent antibacterial activity against resistant bacterial pathogens

The Journal of Antibiotics volume 70, pages 832844 (2017) | Download Citation


The emergence of drug resistance in bacterial pathogens is a growing clinical problem that poses difficult challenges in patient management. To exacerbate this problem, there is currently a serious lack of antibacterial agents that are designed to target extremely drug-resistant bacterial strains. Here we describe the design, synthesis and antibacterial testing of a series of 40 novel indole core derivatives, which are predicated by molecular modeling to be potential glycosyltransferase inhibitors. Twenty of these derivatives were found to show in vitro inhibition of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus. Four of these strains showed additional activity against Gram-negative bacteria, including extended-spectrum beta-lactamase producing Enterobacteriaceae, imipenem-resistant Klebsiella pneumoniae and multidrug-resistant Acinetobacter baumanii, and against Mycobacterium tuberculosis H37Ra. These four compounds are candidates for developing into broad-spectrum anti-infective agents.

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This work was supported by National Natural Science Foundation of China (81460538, 81660588) given to WH; IPSR/RMC/UTARRF/2015-C1/NO3 awarded to YFN by Universiti Tunku Abdul Rahman (UTAR), Kuala Lumpur, Malaysia; and University of Malaya-MOHE High Impact Research grant (UM.C/625/1/HIR/MOHE/DENT/22) given to ICP. The authors would like to thank Dr Charles Laughton at University of Nottingham, UK for offering the access to the computing facilities.

Author information


  1. School of Chemistry and Chemical Engineering, Beifang University of Nationalities, Yinchuan, PR China

    • Wei Hong
  2. Logistics University of the China Armed Police Force, Tianjin, PR China

    • Jingyang Li
  3. School of Pharmacy, Ningxia Medical University, Yinchuan, PR China

    • Zhe Chang
    • , Xiaoli Tan
    • , Hao Yang
    • , Yifan Ouyang
    •  & Hao Wang
  4. School of Basic Medicine, Ningxia Medical University, Yinchuan, PR China

    • Yanhui Yang
  5. Department of Pre-Clinical Sciences, Faculty of Medicine and Health Sciences, Universiti Tunku Abdul Rahman, Selangor, Malaysia

    • Sargit Kaur
    •  & Yun Fong Ngeow
  6. Department of Oral Biology and Biomedical Sciences and Oral Cancer Research and Coordinating Centre, Faculty of Dentistry, University of Malaya, Kuala Lumpur, Malaysia

    • Ian C Paterson
  7. Key Laboratory of Hui Ethnic Medicine Modernization, Ministry of Education, Ningxia Medical University, Yinchuan, PR China

    • Hao Wang


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Competing interests

The authors declare no conflict of interest.

Corresponding authors

Correspondence to Wei Hong or Yun Fong Ngeow or Hao Wang.

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