An update on benzofuran inhibitors: a patent review

ABSTRACT

Introduction: Benzofuran is a fundamental unit in numerous bioactive heterocycles. They have attracted chemists and medical researchers due to their broad range of biological activity, where some of them possess unique anticancer, antitubercular, antidiabetic, anti-Alzheimer and anti-inflammatory properties. The benzofuran nucleus is present in a huge number of bioactive natural and synthetic compounds. Benzofuran derivatives have potent applications in pharmaceuticals, agriculture, and polymers. The recent developments considering the biological activities of benzofuran compounds are reported. They have a vital role as pronounced inhibitors against a number of diseases, viruses, fungus, microbes, and enzymes.

Areas covered: This review covers the recent developments of biological activities of benzofurans during the period 2014–2019. The covered areas here comprised antimicrobial, anti-inflammatory, antitumor, antitubercular, antidiabetic, anti-Alzheimer, antioxidant, antiviral, vasorelaxant, anti-osteoporotic and enzyme inhibitory activities.

Expert opinion: In addition to the already commercialized 34 benzofurans-based drugs in the market, this chapter outlines several potent benzofuran derivatives that may be useful as potential pro-drugs. It is also focused on providing details of SAR and the effect of certain functional groups on the activity of the benzofuran compounds. The presence of -OH, -OMe, sulfonamide, or halogen contributed greatly to increasing the therapeutic activities comparing with reference drugs.

KEYWORDS:

• Benzofurans
• natural products
• anti-inflammatory
• antimicrobial
• antitumor
• antiviral

Article highlights

• Benzofuran compounds are included in more than 30 commercial drugs in the market.

• Several benzofurans reported here are potent and selective anti-inflammatory, antibacterial, anticancer, anti-HCV and herbicidal agents.

• A number of benzofuran derivatives are interesting drug candidates (e.g. antidiabetic, anticancer and antituberculosis) where they showed better activity than the corresponding reference drugs.

• SAR revealed that presence of certain functional groups is effective for enhancement of the pharmacological activity of benzofurans.

• This updated collection (2014-2019) is of great interest for chemistry, medicinal and pharmaceutical researchers.

• Most of the reported benzofurans showed nanomolar potency against wide range of diseases.

• There are 30 patents among 148 references are cited herein covering 16 biological areas.

This box summarizes key points contained in the article.

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 paper was not funded.