Therapeutic Potential of Naturally Occurring Benzofuran Derivatives and Hybrids of Benzofurans with other Pharmacophores as Antibacterial Agents

Gram-positive and Gram-negative pathogens are able to evade the host immune system, persist within the human host, and lead to severe disease and even death. At present, bacterial infections are one of the leading causes of morbidity and mortality across the world. The development of novel antibacterial agents still represents a challenging endeavor, which is mainly attributed to the continuous emergence of more virulent and drug-resistant pathogens. Benzofuran constitutes the core of diverse pharmacologically active compounds, and there are a variety of approved benzofuranbased drugs in the market or currently going through different clinical phases or registration statuses. Benzofurans could exert antibacterial activity through various mechanisms and possess pronounced activity; therefore, benzofuran is a useful skeleton for the discovery of novel antibacterial agents. This review focuses on the recent advancement of naturally occurring benzofuran derivatives and hybrids of benzofurans with other pharmacophores as antibacterial agents, covering articles published between January 2015 and July 2021. The chemical structures and structure-activity relationships are also discussed.

Automated summary

Gram-positive and Gram-negative pathogens pose a significant threat to human health, resulting in severe diseases and high mortality rates. Developing novel antibacterial agents remains challenging due to the emergence of more virulent and drug-resistant pathogens. Benzofuran, with its diverse pharmacological activities, shows promise as a potential scaffold for discovering new antibacterial agents. This review focuses on the recent advancements in naturally occurring benzofuran derivatives and hybrids of benzofurans with other pharmacophores as antibacterial agents, providing valuable insights into their chemical structures and structure-activity relationships.