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Enaminones as building blocks in drug development: Recent advances in their chemistry, synthesis, and biological properties
Tetrahedron ( IF 2.1 ) Pub Date : 2021-02-04 , DOI: 10.1016/j.tet.2021.131984
Isis J. Amaye , Rhashanda D. Haywood , Edelquine M. Mandzo , Jeremy J. Wirick , Patrice L. Jackson-Ayotunde

The enaminone scaffold is a versatile building block used in organic synthesis. The amine – alkene – carbonyl conjugated system, having both nucleophilic and electrophilic characteristics, allows for a highly reactive center, that can serve as a pharmacophore for molecules in drug development. Analogs with this moiety have an array of pharmacological responses such as antiviral, anti-inflammatory, antitumor, anticancer and anticonvulsant activities. Herein, this review provides insight of current synthetic methodologies that employ enaminones as intermediates and their preparations. Structure activity relationship studies of various enaminone analogs will be examined in this review as well.



中文翻译:

烯胺酮作为药物开发的基础:其化学,合成和生物学特性的最新进展

烯胺骨架是有机合成中使用的通用构建基块。具有亲核和亲电特性的胺-烯烃-羰基共轭体系可形成高反应活性中心,可作为药物开发中分子的药效团。具有该部分的类似物具有一系列药理反应,例如抗病毒,抗炎,抗肿瘤,抗癌和抗惊厥活性。在本文中,本综述提供了使用烯胺酮作为中间体及其制备方法的当前合成方法的见解。各种烯胺类似物的结构活性关系研究也将在本综述中进行研究。

更新日期:2021-03-16
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