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Issue 117, 2015
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Benzofuran: an emerging scaffold for antimicrobial agents

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Resistance to antibiotics is a major global problem and there is an urgent need to develop new therapeutic agents. Although many classes of active compounds have been established as efficient derivatives in diverse fields of antimicrobial therapy, they have not yet found wide application against a few deadly microbes. In recent years, compounds have been developed that have solved some of the problems posed; for example improved bioavailability is one of the targets achieved with most of the more recent compounds, allowing for once-daily dosing. Benzofuran and its derivatives are found to be suitable structures, existing widely in natural products and unnatural compounds with a wide range of biological and pharmacological applications; thus, considerable attention has been focused on the discovery of new drugs in the fields of drug invention and development. Some benzofuran derivatives, such as psoralen, 8-methoxypsoralen and angelicin have been used in the treatment of skin diseases such as cancer or psoriasis. The unique structural features of benzofuran and its wide array of biological activities make it a privileged structure in the field of drug discovery, especially in the search for efficient antimicrobial candidates. Recently, this scaffold has emerged as a pharmacophore of choice for designing antimicrobial agents that are active toward different clinically approved targets. To pave the way for future research, there is a need to collect the latest information in this promising area. In the present review, we collated the published reports on this versatile core to provide a deeper insight, so that its full therapeutic potential can be utilized for the treatment of microbial diseases. This study systematically provides a comprehensive report on current developments in benzofuran-based compounds as antimicrobial agents and is also helpful for the researchers working on a substitution pattern around the nucleus, with an aim to help medicinal chemists to develop structure activity relationships (SAR) on these derivatives as antimicrobial drugs.

Graphical abstract: Benzofuran: an emerging scaffold for antimicrobial agents

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Article information

06 Oct 2015
27 Oct 2015
First published
27 Oct 2015

RSC Adv., 2015,5, 96809-96828
Article type
Review Article
Author version available

Benzofuran: an emerging scaffold for antimicrobial agents

A. Hiremathad, M. R. Patil, C. K. R., K. Chand, M. A. Santos and R. S. Keri, RSC Adv., 2015, 5, 96809
DOI: 10.1039/C5RA20658H

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