Substituted tetralones have played a substantial role in organic synthesis due to their strong reactivity and suitability as a starting material for a range of synthetic heterocyclic compounds, pharmaceuticals along with biological activities as well as precursors of many natural products and their derivatives. Many α-tetralone derivatives are building blocks that have been used in the synthesis of therapeutically functional compounds like some antibiotics, antidepressants, acetylcholinesterase inhibitors effective for treating Alzheimer’s disease and alkaloids possessing antitumor activity. In this review, there has been an attempt to explore the small molecule library having an α-tetralone scaffold along with their diverse biological activities. Structural features of α- tetralone derivatives responsible for potential therapeutic applications are also described.

取代的四氢萘酮在有机合成中起着重要作用，因为它们具有很强的反应性和适用性，可作为一系列合成杂环化合物，药物以及生物活性以及许多天然产物及其衍生物的前体的起始原料。许多α-四氢萘酮衍生物是已被用于合成治疗功能化合物的结构单元，如某些抗生素，抗抑郁药，有效治疗阿尔茨海默氏病的乙酰胆碱酯酶抑制剂和具有抗肿瘤活性的生物碱。在这篇综述中，已经尝试探索具有α-四氢萘酮支架及其小生物活性的小分子文库。