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Morpholine As a Scaffold in Medicinal Chemistry: An Update on Synthetic Strategies.
ChemMedChem ( IF 3.6 ) Pub Date : 2020-02-04 , DOI: 10.1002/cmdc.201900682
Ariadni Tzara 1 , Dimitrios Xanthopoulos 1 , Angeliki P Kourounakis 1
Affiliation  

Morpholine is a frequently used heterocycle in medicinal chemistry and a privileged structural component of bioactive molecules. This is mainly due to its contribution to a plethora of biological activities as well as to an improved pharmacokinetic profile of such bioactive molecules. The synthesis of morpholines is a subject of much study due to their biological and pharmacological importance, with the last such review being published in 2013. Here, an overview of the main approaches toward morpholine synthesis or functionalization is presented, emphasizing on novel work which has not been reviewed so far. This review is an update on synthetic strategies leading to easily accessible libraries of bioactives which are of interest for drug discovery projects.

中文翻译:

吗啉作为药物化学中的支架:合成策略的最新进展。

吗啉是药物化学中常用的杂环,是生物活性分子的优先结构组分。这主要是由于其对过多的生物活性的贡献以及这种生物活性分子的改善的药代动力学特征。由于吗啉的生物学和药理重要性,因此是许多研究的主题,最近的综述于2013年发表。在这里,概述了吗啉合成或功能化的主要方法,重点介绍了到目前为止尚未进行审查。这篇综述是对合成策略的更新,该策略导致了易于开发的生物活性物质库,这对于药物发现项目很重要。
更新日期:2020-02-12
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