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The benzofuran moiety constitutes a main component of enormous biologically active natural and synthetic heterocycles. Such heterocycles have distinctive therapeutic potential and are employed in various clinical drugs. A number of publications have dealt with the synthesis and extraction of benzofuran-based heterocycles to investigate their antimicrobial potential. This review describes the antimicrobial activity of various natural and synthetic benzofuran scaffolds. The antimicrobial activity of benzofurans is thoroughly investigated against several bacterial (Gram-positive and Gram-negative) and fungal microorganisms compared with several reference antibiotic drugs. The effects of the electronic nature of substituents on the activity of benzofurans through SAR study were reported. This article also highlights the recent natural and synthetic benzofuran-based organic molecules between 2019–2022 that have had success in terms of their antimicrobial activity. Many of the described benzofurans are promising candidates as antimicrobial agents based on their activity. Most used antibiotics target infections caused by the gram-positive pathogen  S. aureus . Interestingly, most of the described benzofurans are promising inhibitors against  S. aureus  with either equipotent or more potent activity than the reference antibiotic drugs. These findings will encourage medicinal chemists to explore these new avenues for human health promotion to reduce suffering.

Benzofuran as a promising scaffold for the synthesis of novel antimicrobial agents