阿尔茨海默病(AD)日益引起全球健康关注。近几十年来,天然和合成色烯酮由于其多靶点潜力而成为有前途的候选药物。天然色烯酮,槲皮素,scopoletin,esculetin,coumestrol,伞形酮,Bergapten,和甲氧沙林(黄曲霉毒素),和含有吖啶等结构的合成色烯酮杂种,4-氨基苯基,3-芳基香豆素,喹啉,1,3,4-恶二唑,1,2,3-三唑,和他克林,已经被探索了它们对抗AD的潜力。用于合成色烯酮杂化物的关键反应包括Perkin和Pechmann缩合。已经报道了色烯酮杂种对几种药物靶标的活性,包括AChE,BuChe,BACE-1和MAO-A/B这篇综述全面探讨了自然,半合成,和合成色烯酮,阐明他们的合成路线,可能的作用方式/药物靶标和结构-活性关系(SAR)。获得的知识为开发针对AD的新的苯并吡喃酮杂种提供了有价值的见解。
Alzheimer\'s disease (AD) presents a growing global health concern. In recent decades, natural and synthetic chromenone have emerged as promising drug candidates due to their multi-target potential. Natural chromenone, quercetin, scopoletin, esculetin, coumestrol, umbelliferone, bergapten, and methoxsalen (xanthotoxin), and synthetic chromenone hybrids comprising structures like acridine, 4-aminophenyl, 3-arylcoumarins, quinoline, 1,3,4-oxadiazole, 1,2,3-triazole, and tacrine, have been explored for their potential to combat AD. Key reactions used for synthesis of chromenone hybrids include Perkin and Pechmann condensation. The activity of chromenone hybrids has been reported against several drug targets, including AChE, BuChE, BACE-1, and MAO-A/B. This review comprehensively explores natural, semisynthetic, and synthetic chromenone, elucidating their synthetic routes, possible mode of action/drug targets and structure-activity relationships (SAR). The acquired knowledge provides valuable insights for the development of new chromenone hybrids against AD.