Recent advances in the design of small molecular drugs with acrylamides covalent warheads

IF 3.3 3区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Luxia Liang , Ze Zhang , Qidong You , Xiaoke Guo
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引用次数: 0

Abstract

In the development of covalent inhibitors, acrylamides warhead is one of the most popular classes of covalent warheads. In recent years, researchers have made different structural modifications to acrylamides warheads, resulting in the creation of fluorinated acrylamide warheads and cyano acrylamide warheads. These new warheads exhibit superior selectivity, intracellular accumulation, and pharmacokinetic properties. Additionally, although ketoamide warheads have been applied in the design of covalent inhibitors for viral proteins, it has not received sufficient attention. Combined with the studies in kinase inhibitors and antiviral drugs, this review presents the structural features and the progression of acrylamides warheads, offering a perspective on future research and development in this field.

Abstract Image

使用丙烯酰胺共价弹头设计小分子药物的最新进展
在共价抑制剂的开发过程中,丙烯酰胺弹头是最受欢迎的一类共价弹头。近年来,研究人员对丙烯酰胺弹头进行了不同的结构改造,创造出了氟化丙烯酰胺弹头和氰基丙烯酰胺弹头。这些新弹头在选择性、细胞内蓄积和药代动力学特性方面都表现出卓越的性能。此外,尽管酮酰胺弹头已被应用于病毒蛋白质共价抑制剂的设计,但尚未引起足够的重视。结合激酶抑制剂和抗病毒药物方面的研究,本综述介绍了丙烯酰胺弹头的结构特点和研究进展,为该领域未来的研究和发展提供了一个视角。
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来源期刊
Bioorganic & Medicinal Chemistry
Bioorganic & Medicinal Chemistry 医学-生化与分子生物学
CiteScore
6.80
自引率
2.90%
发文量
413
审稿时长
17 days
期刊介绍: Bioorganic & Medicinal Chemistry provides an international forum for the publication of full original research papers and critical reviews on molecular interactions in key biological targets such as receptors, channels, enzymes, nucleotides, lipids and saccharides. The aim of the journal is to promote a better understanding at the molecular level of life processes, and living organisms, as well as the interaction of these with chemical agents. A special feature will be that colour illustrations will be reproduced at no charge to the author, provided that the Editor agrees that colour is essential to the information content of the illustration in question.
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