Escuela de Ciencias Química, Facultad de Ciencias, Universidad Pedagógica y Tecnológica de Colombia, Avenida Central del Norte, Tunja 150003, Colombia.
Research Group of Heterocyclic Compounds, Department of Chemistry, Universidad del Valle, A.A. 25360, Cali 76001, Colombia.
Molecules. 2022 Jul 23;27(15):4723. doi: 10.3390/molecules27154723.
Pyrazole and its derivatives are considered a privileged -heterocycle with immense therapeutic potential. Over the last few decades, the pot, atom, and step economy (PASE) synthesis of pyrazole derivatives by multicomponent reactions (MCRs) has gained increasing popularity in pharmaceutical and medicinal chemistry. The present review summarizes the recent developments of multicomponent reactions for the synthesis of biologically active molecules containing the pyrazole moiety. Particularly, it covers the articles published from 2015 to date related to antibacterial, anticancer, antifungal, antioxidant, α-glucosidase and α-amylase inhibitory, anti-inflammatory, antimycobacterial, antimalarial, and miscellaneous activities of pyrazole derivatives obtained exclusively via an MCR. The reported analytical and activity data, plausible synthetic mechanisms, and molecular docking simulations are organized in concise tables, schemes, and figures to facilitate comparison and underscore the key points of this review. We hope that this review will be helpful in the quest for developing more biologically active molecules and marketed drugs containing the pyrazole moiety.
吡唑及其衍生物被认为是一种具有巨大治疗潜力的特权杂环。在过去的几十年中，多组分反应（MCRs）的 pot、atom、and step economy（PASE）合成吡唑衍生物在药物和药物化学领域越来越受欢迎。本文综述了近年来多组分反应合成含有吡唑部分的生物活性分子的最新进展。特别是，它涵盖了自 2015 年以来发表的与通过 MCR 获得的吡唑衍生物的抗菌、抗癌、抗真菌、抗氧化、α-葡萄糖苷酶和α-淀粉酶抑制、抗炎、抗分枝杆菌、抗疟原虫和杂项活性相关的文章。报告的分析和活性数据、合理的合成机制和分子对接模拟以简洁的表格、方案和图形进行组织，以方便比较并强调本综述的要点。我们希望本综述有助于开发更多具有生物活性的分子和含有吡唑部分的上市药物。
