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Benzofuran: A Key Heterocycle - Ring Closure And Beyond

Author(s):

Andiappan Lavanya, Kilambi Narasimhan* and Vediappen Padmini   Pages 1 - 52 ( 52 )

Abstract:


The benzofuranyl motif is present in compounds exhibiting various medicinal properties and non-drug applications as well. 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. A 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 their interesting biological activities and commercial utilities, a review on the synthetic aspects of this privileged scaffold is attempted here. For the benefit of natural product-based drug discovery, the source of these derivatives, extraction and reported biological activities are also outlined in this review.

Keywords:

Benzofuran derivatives, ring-closure, drug and non-drug application, synthetic-strategieBenzofuran derivatives, synthetic-strategies

Affiliation:

Department of Training and Development, Orchid Pharma Ltd, 138-149, SIDCO Industrial Estate, Alathur, Chennai-603 110, Tamil Nadu, Department of Training and Development, Orchid Pharma Ltd, 138-149, SIDCO Industrial Estate, Alathur, Chennai-603 110, Tamil Nadu, Department of Organic Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai 625021, Tamil Nadu



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