Benzothiazole-based Compounds in Antibacterial Drug Discovery

Curr Med Chem. 2018;25(38):5218-5236. doi: 10.2174/0929867324666171009103327.

Abstract

Numerous compounds with a benzothiazole scaffold that have been described in the literature show promising activities against several Gram-positive and Gramnegative bacteria, and also against Mycobacterium tuberculosis. Benzothiazole-based antibacterial compounds bind to different biological targets in bacterial cells and have been shown to be inhibitors of enzymes that are important for essential processes in the bacterial cells, such as cell-wall synthesis, cell division, and DNA replication, or are important for different biosynthetic pathways of essential compounds in bacterial cells, such as the biosynthesis of histidine and biotin. This review focuses on the antibacterial potential of benzothiazole-based compounds, in terms of their specific interactions with targets in bacterial cells. We assess the importance of the benzothiazole scaffold in the discovery of new antibacterial compounds, the potential of benzothiazole-based compounds against resistant bacterial strains, optimization of their antibacterial activity, and the future perspectives of benzothiazole-based antibacterials.

Keywords: Benzothiazole; antibacterial; antibiofilm; antimycobacterial; bacterial resistance; molecular target..

Publication types

  • Review

MeSH terms

  • Animals
  • Antitubercular Agents / pharmacology
  • Antitubercular Agents / therapeutic use*
  • Bacterial Infections / drug therapy*
  • Bacterial Proteins / antagonists & inhibitors
  • Benzothiazoles / pharmacology
  • Benzothiazoles / therapeutic use*
  • Drug Discovery*
  • Enzyme Inhibitors / pharmacology
  • Enzyme Inhibitors / therapeutic use
  • Gram-Negative Bacteria / drug effects
  • Gram-Positive Bacteria / drug effects
  • Humans
  • Microbial Sensitivity Tests

Substances

  • Antitubercular Agents
  • Bacterial Proteins
  • Benzothiazoles
  • Enzyme Inhibitors