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1,4-苯并二恶烷:医药化学中一种常绿、多功能的支架:其在药物设计中的最新应用综述。

1,4-Benzodioxane, an evergreen, versatile scaffold in medicinal chemistry: A review of its recent applications in drug design.

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Milano, Via Mangiagalli 25, I-20133, Milano, Italy.

Dipartimento di Scienze Farmaceutiche, Università di Milano, Via Mangiagalli 25, I-20133, Milano, Italy.

出版信息

Eur J Med Chem. 2020 Aug 15;200:112419. doi: 10.1016/j.ejmech.2020.112419. Epub 2020 May 11.

Abstract

1,4-Benzodioxane has long been a versatile template widely employed to design molecules endowed with diverse bioactivities. Its use spans the last decades of medicinal chemistry until today concerning many strategies of drug discovery, not excluding the most advanced ones. Here, more than fifty benzodioxane-related lead compounds, selected from recent literature, are presented showing the different approaches with which they have been developed. Agonists and antagonists at neuronal nicotinic, α adrenergic and serotoninergic receptor subtypes and antitumor and antibacterial agents form the most representative classes, but a variety of other biological targets are addressed by benzodioxane-containing compounds.

摘要

1,4-苯并二恶烷长期以来一直是一种用途广泛的模板,广泛用于设计具有多种生物活性的分子。它在过去几十年的药物化学中被使用,直到今天仍涉及到许多药物发现策略,包括最先进的策略。在这里,从最近的文献中选择了五十多种与苯并二恶烷相关的先导化合物进行介绍,展示了它们的不同开发方法。 神经元烟碱型、α肾上腺素能和 5-羟色胺能受体亚型的激动剂和拮抗剂以及抗肿瘤和抗菌剂是最具代表性的类别,但含苯并二恶烷的化合物还针对多种其他生物靶点。

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