Therapeutic significance of quinolines: a patent review (2013-2015)

ABSTRACT

Introduction: Quinoline is a versatile bicyclic heterocyclic scaffold with immense therapeutic potential. Some of the compounds containing quinoline nucleus are agents of choice for the treatment of various ailments, particularly cancer and malaria. Furthermore, several quinoline derivatives exhibit a broad spectrum of antimicrobial, anti-inflammatory, and antidiabetic activities, quite a few of which are under clinical investigation to combat potentially lethal diseases/disorders.

Areas covered: The present review summarizes inventions developed towards finding new chemotherapeutic agents based on the quinoline skeleton. It presents an outline of patents filed between 2013 and 2015, relating to the anticancer, antimicrobial, anti-inflammatory and other biological activities exhibited by quinoline derivatives.

Expert opinion: Several molecules containing quinoline skeleton are clinically significant drugs, extensively used for the treatment of various human diseases/disorders. The clinical success of some of these compounds and the versatile character of the quinoline nucleus attracted medicinal chemists in the development of newer chemotherapeutic agents. The considerably high number of patents filed in a relatively short period of time indicates the increasing importance of this pharmacophore. The development of facile synthetic strategies is anticipated to facilitate the generation of chemical libraries that could serve as a source of new chemical entities.

KEYWORDS:

• Quinoline
• anticancer
• antimicrobial
• anti-inflammatory
• anti-diabetic

Article highlights

• Recently filed patents on quinoline skeleton discussing its therapeutic significance are described.

• Some quinoline derivatives, particularly kinase inhibitors, are claimed as probable medications for cancer.

• Anticancer potential of some other quinoline derivatives is discussed.

• Quinoline derivatives are also shown to kill disease-causing pathogens and are claimed to be useful in the treatment of infectious diseases.

• Some quinoline derivatives are claimed to possess anti-inflammatory activity owing to their ability to inhibit RORγt.

• Patents describing the use of quinoline congeners for the treatment of several other diseases such as diabetes, neurological disorders etc are also discussed.

This box summarizes key points contained in the article.

Acknowledgment

The author thanks Prof. M. S. C. Pedras, Department of Chemistry, University of Saskatchewan for support and current position in NSERC funded project.

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 was not funded.