State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
Bioorg Med Chem. 2024 Oct 1;112:117902. doi: 10.1016/j.bmc.2024.117902. Epub 2024 Aug 30.
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.
在共价抑制剂的发展中，丙烯酰胺弹头是最受欢迎的共价弹头之一。近年来，研究人员对丙烯酰胺弹头进行了不同的结构修饰，从而产生了氟化丙烯酰胺弹头和氰基丙烯酰胺弹头。这些新的弹头表现出更高的选择性、细胞内积累和药代动力学特性。此外，尽管酮酰胺弹头已应用于病毒蛋白共价抑制剂的设计，但它并未受到足够的重视。结合激酶抑制剂和抗病毒药物的研究，本文综述了丙烯酰胺弹头的结构特征和进展，为该领域的未来研究和发展提供了一个视角。
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