School of Chemical Science and Engineering, Yachay University for Experimental Technology and Research (Yachay Tech), Yachay City of Knowledge, Urcuqui 100119, Ecuador.
Institute for Research in Biomedicine, Barcelona Science Park, 08028 Barcelona, Spain.
Molecules. 2022 Aug 9;27(16):5070. doi: 10.3390/molecules27165070.
3,4-Dihydro-2(1)-pyridones () and their derivatives are privileged structures, which has increased their relevance due to their biological activity in front of a broad range of targets, but especially for their importance as synthetic precursors of a variety of compounds with marked biological activity. Taking into account the large number of contributions published over the years regarding this kind of heterocycle, here, we presented a current view of 3,4-dihydro-2(1)-pyridones (). The review includes general aspects such as those related to nomenclature, synthesis, and biological activity, but also highlights the importance of as building blocks of other relevant structures. Additional to the conventional multicomponent synthesis of the mentioned heterocycle, nonconventional procedures are revised, demonstrating the increasing efficiency and allowing reactions to be carried out in the absence of the solvent, becoming an important contribution to green chemistry. Biological activities of , such as vasorelaxant, anti-HIV, antitumor, antibacterial, and antifungal, have demonstrated this heterocycle's potential in medicinal chemistry.
3,4-二氢-2(1H)-吡啶酮()及其衍生物是一种重要的结构,由于其对广泛的靶标具有生物活性,尤其是作为多种具有显著生物活性的化合物的合成前体的重要性,因此增加了它们的相关性。考虑到多年来发表的大量关于这种杂环的论文,我们在这里对 3,4-二氢-2(1H)-吡啶酮()进行了综述。综述涵盖了一般性方面,如命名法、合成和生物活性等,但也强调了作为其他相关结构构建模块的重要性。除了常规的多组分合成方法外,还对非传统方法进行了修订,证明了这些方法的效率不断提高,并且可以在没有溶剂的情况下进行反应,这对绿色化学做出了重要贡献。3,4-二氢-2(1H)-吡啶酮的生物活性,如血管舒张、抗 HIV、抗肿瘤、抗菌和抗真菌活性,证明了这种杂环在药物化学中的潜力。