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Benzopyrone, a privileged scaffold in drug discovery: An overview of FDA‐approved drugs and clinical candidates
Medicinal Research Reviews ( IF 13.3 ) Pub Date : 2024-03-27 , DOI: 10.1002/med.22032
Venu Sharma 1 , Ankita Sharma 1, 2 , Bhagyashri N. Wadje 3 , Sandip B. Bharate 1, 2, 3
Affiliation  

Natural products have always served as an important source of drugs for treating various diseases. Among various privileged natural product scaffolds, the benzopyrone class of compounds has a substantial presence among biologically active compounds. One of the pioneering anticoagulant drugs, warfarin approved in 1954 bears a benzo‐α‐pyrone (coumarin) nucleus. The widely investigated psoriasis drugs, methoxsalen, and trioxsalen, also contain a benzo‐α‐pyrone nucleus. Benzo‐γ‐pyrone (chromone) containing drugs, cromoglic acid, and pranlukast were approved as treatments for asthma in 1982 and 2007, respectively. Numerous other small molecules with a benzopyrone core are under clinical investigation. The present review discusses the discovery, absorption, distribution, metabolism, excretion properties, and synthetic approaches for the Food and Drug Administration‐approved and clinical‐stage benzopyrone class of compounds. The role of the pyrone core in biological activity has also been discussed. The present review unravels the potential of benzopyrone core in medicinal chemistry and drug development.

中文翻译:

苯并吡喃酮,药物发现中的一种特殊支架:FDA 批准的药物和临床候选药物概述

天然产物一直是治疗多种疾病的重要药物来源。在各种独特的天然产物支架中,苯并吡喃酮类化合物在生物活性化合物中大量存在。华法林是开创性的抗凝药物之一,于 1954 年获得批准,带有苯并-α-吡喃酮(香豆素)核。广泛研究的牛皮癣药物甲氧沙林和三氧沙林也含有苯并-α-吡喃酮核。含有苯并-γ-吡喃酮(色酮)的药物、色甘酸和普仑司特分别于 1982 年和 2007 年被批准用于治疗哮喘。许多其他具有苯并吡喃酮核心的小分子正在临床研究中。本综述讨论了美国食品和药物管理局批准的临床阶段苯并吡喃酮类化合物的发现、吸收、分布、代谢、排泄特性和合成方法。还讨论了吡喃酮核心在生物活性中的作用。本综述揭示了苯并吡喃酮核心在药物化学和药物开发中的潜力。
更新日期:2024-03-27
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