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Pyridones in drug discovery: Recent advances
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2021-02-18 , DOI: 10.1016/j.bmcl.2021.127849
Yun Zhang 1 , Andrew Pike 2
Affiliation  

Pyridones have been utilized as privileged scaffolds in drug discovery. Some of the important roles where this class of heterocycles have found utility in medicinal chemistry include the ability to 1) serve both as a hydrogen bond acceptor and/or a donor; 2) act as a bioisostere for amides, phenyls, pyridines and other nitrogen- or oxygen-containing heterocycles; and 3) impact a target drug molecule’s lipophilicity, aqueous solubility and metabolic stability. Detailed discussions of recent advances in their utilization as nonpeptidic mimics and as kinase hinge binding motifs are included. Selected literature examples published from the past twenty years where pyridones have been employed as bioisosteres for phenyls, pyridines, pyridine N-oxides and phenol rings are provided. In addition, this review summarizes the current understanding of possible reactive metabolites related to the pyridone structure.



中文翻译:

药物发现中的吡啶酮:最新进展

吡啶酮已被用作药物发现中的特权支架。这类杂环在药物化学中的一些重要作用包括:1) 作为氢键受体和/或供体;2) 作为酰胺、苯基、吡啶和其他含氮或含氧杂环的生物等排体;3) 影响目标药物分子的亲脂性、水溶性和代谢稳定性。详细讨论了它们在用作非肽模拟物和激酶铰链结合基序方面的最新进展。过去 20 年出版的精选文献示例,其中吡啶酮被用作苯基、吡啶、吡啶N 的生物电子等排体- 提供了氧化物和酚环。此外,本综述总结了目前对与吡啶酮结构相关的可能反应性代谢物的理解。

更新日期:2021-02-25
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