Benzofuran: A Key Heterocycle - Ring Closure And Beyond

The benzofuranyl motif present in compounds exhibits various medicinal properties and non-drug applications. These derivatives are naturally occurring compounds or synthetic materials, which cover a broad spectrum of pharmacological activities like anti-inflammatory, anti-diabetic, anti- depressant, anti-HIV, anti-microbial, anti-proliferative, anti-convulsant, cytotoxic, analgesic, etc. Few of the commercially interesting compounds from this class are, ailanthoidol (anti-inflammatory), amiodarone, dronedarone, celivarone (anti-arrhythmic), bufuralol (muscular airways relaxant), morphine, 5-(2-aminopropyl)benzofuran; 5-APB, 6-(2-aminopropyl)benzofuran; 6-APB (CNS), rifampicin (antibiotic), etc., whereas, some of the non-drug applications are in perfumery industry (bergapten) and as tannin activators in sunscreen preparations (psoralen, 8-methoxypsoralen, and angelicin). Considering these interesting biological activities and commercial utilities, a review on the synthetic aspects of this privileged scaffold was attempted. For the benefit of natural product-based drug discovery, available sources of these derivatives, extraction process and reported biological activities have also been outlined in this review.