Therapeutic Potential of Naturally Occurring Benzofuran Derivatives and Hybrids of Benzofurans with other Pharmacophores as Antibacterial Agents

Abstract

: Gram-positive and Gram-negative pathogens are able to evade the host immune system, persist within the human host, and lead to severe disease and even death. At present, bacterial infections are one of the leading causes of morbidity and mortality across the world. Development of novel antibacterial agents still represents a challenging endeavor, which is mainly attributed to the continuous emergence of more virulent and drug-resistant pathogens. Benzofuran constitutes the core of diverse pharmacologically active compounds, and there are a variety of approved benzofuran-based drugs in the market or currently going through different clinical phases or registration statuses. Benzofurans could exert antibacterial activity through various mechanisms and possess pronounced activity, so benzofuran is a useful skeleton for the discovery of novel antibacterial agents. This review focuses on the recent advancement of naturally occurring benzofuran derivatives and hybrids of benzofurans with other pharmacophores as antibacterial agents, covering articles published between January 2015 and July 2021. The chemical structures and structure-activity relationships are also discussed.

Synthesis of novel conjugated benzofuran-triazine derivatives: Antimicrobial and in-silico molecular docking studies

“…The reaction then continued at this temperature for 5 h until TLC confirmed the reaction had been completed. Finally, diluted HCl (1:5, 3 mL) was added to the reaction mixture and the desired crude product was extracted with chloroform (yield: 65%) [ 26 ].…”

A Comprehensive Review on Benzofuran Synthesis Featuring Innovative and Catalytic Strategies

“…Benzofuran derivatives have been found to be active against bacterial, − viral, , inflammatory, and protozoal diseases . For example, diabetes, HIV, tuberculosis, epilepsy, and Alzheimer’s disease are some of the most common and widely occurring diseases, against which benzofuran derivatives have been known to play a therapeutic role.…”

Discovery of New Heterocyclic/Benzofuran Hybrids as Potential Anti-Inflammatory Agents: Design, Synthesis, and Evaluation of the Inhibitory Activity of Their Related Inflammatory Factors Based on NF-κB and MAPK Signaling Pathways

“…Benzofuran compounds are a class of compounds that are ubiquitous in nature, which possess a wide range of biological applications, such as antioxidant [ 14 ], anti-inflammatory [ 15 ], antitumor [ 16 ], antibacterial [ 17 ], antiviral [ 18 ], antituberculosis [ 19 ], antidiabetic [ 20 ] and antidepression [ 21 , 22 ], etc. Various nitrogen containing heterocyclic fragments such as piperazine, tetrazole and imidazole were reported to exhibit anti-inflammatory properties [ 23 , 24 , 25 , 26 ].…”