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

ABSTRACT

Introduction

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.

Areas covered

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.

Expert opinion

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.

KEYWORDS:

• Antimicrobial activity
• benzofuran
• antibiotics
• heterocycles
• natural products

Article highlights

• Several benzofuran scaffolds are employed in a number of clinically approved drugs.

• A benzofuran nucleus is a key component in a wide-range of naturally occurring organic compounds.

• Many natural and synthetic benzofuran derivatives have promise as potential antimicrobial agents due to their superior activity compared with the reference drugs and showed high potency against panels of microorganisms on a nanomolar scale.

• SAR has revealed a pivotal role for some functional groups to enhance the pharmacological properties of benzofurans.

• The authors believe that the findings herein will encourage medicinal chemists to explore new avenues for human health promotion and reducing suffering.

Declaration of Interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer Disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This manuscript was not funded.