Current Organic Synthesis ( IF 1.8 ) Pub Date : 2021-10-31 , DOI: 10.2174/1570179418666210301122322 Nitin K Jadhav 1 , Balkrishna R Kale 2 , Mohammad S Alam 2 , Vishwas B Gaikwad 1 , Virendra Prasad 3 , Raju R Kale 1
Heterocycles are the main structural motif of DNA and RNA and play a crucial role in various chemical reactions of metabolisms. Therefore, heterocyclic compounds show good physiological and pharmacological properties. Coumarin and pyrazole scaffolds are present in many commercial drug molecules and natural products. This review overviews the progress made in the synthesis and functionalization of the coumarin- pyrazole hybrid heterocycle. It also includes discussion on the possible reactive sites of heterocycles, functionalization, and mechanistic pathways to incorporate pyrazole pharmacophore unit in synthesis. Several synthesis and biological studies reveal that the combination of the coumarin-pyrazole moiety is a prominent structural motif to find lead compounds in drug discovery.
中文翻译:
香豆素-吡唑支架的合成和功能化:最新发展、挑战和机遇
杂环是 DNA 和 RNA 的主要结构基序,在代谢的各种化学反应中起着至关重要的作用。因此,杂环化合物表现出良好的生理和药理特性。香豆素和吡唑支架存在于许多商业药物分子和天然产品中。本综述概述了香豆素-吡唑杂环杂环的合成和功能化方面的进展。它还包括对杂环的可能反应位点、功能化和在合成中结合吡唑药效团单元的机制途径的讨论。几项合成和生物学研究表明,香豆素-吡唑部分的组合是在药物发现中寻找先导化合物的重要结构基序。