Coumarin derivatives: an updated patent review (2015-2016)

ABSTRACT

Introduction: Coumarins belong to the benzopyrone family. They are naturally plant-derived or synthetically obtained substances, presenting a wide variety of biological activities, offering an extented therapeutic profile. Their structural characteristics correlated to physicochemical properties define their pleiotropic biological responses.

Areas covered in this review: Recent patent publications (2015–2016), describing coumarins and their derivatives are analyzed. Synthesis, biological evaluations in vitro /in vivo e.g. antiviral, anticancer, cytotoxic, antioxidant, anti-inflammmatory protocols are included. Furthermore, several pharmaceutical applications and pharmaceutical compositions are also described.

Expert opinion: Several synthetic coumarins, hybrids and derivatives (azoles, sulfonyl, furazan, pyrazole etc) have been found to possess promising anticancer, antitumor anti-proliferative activities. Their clinical evaluation will be critical to assess therapeutic utility. The compounds for which the mechanism of action is well defined can serve as lead compounds for the design of new more potent molecules.

KEYWORDS:

• Anti-Alzheimer
• anticancer
• antimicrobial
• antioxidant
• antiviral
• MAO inhibitors
• coumarin
• cytotoxicity

Article highlights

• Coumarins are characterized as α-benzopyrones

• New and known coumarin derivatives have been synthesized or isolated from natural sources.

• Coumarins inhibit various different target proteins and enzymes.

• A huge number of coumarins present antioxidant, anti-inflammatory, cytotoxic, antitumor, anticancer, antibacterial, antiviral, anti-HIV and anti-Alzheimer activities.

• Coumarins can be used as α-glucosidase, melanin, aromatase, tyrosinase and MAO inhibitors and as nematicides

• Coumarin derivatives applied for skin diseases, arthropathy, hepatitis, imaging and cerebral ischemia and Alzheimer’s disease.

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.

Additional information

Funding

This paper has not been funded