State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, China.
State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, China.
Eur J Med Chem. 2022 Dec 5;243:114739. doi: 10.1016/j.ejmech.2022.114739. Epub 2022 Sep 7.
The fusion of pyrazole scaffold with other skeletons creates a class of attractive molecules, demonstrating significant biological and chemical potentiality in the development of medicinal chemistry. Over the past few decades, numerous biologically active molecules featuring fused pyrazole moieties have been excavated and synthesized, some of which represented by sildenafil have been marketed as drugs, and the biological importance together with chemical synthesis strategies of fused pyrazole compounds, including structural modification based on lead compounds, have been steadily progressing. In this review, we focused our attention on the biological importance of fused pyrazoles and highlighted recent progress in the synthesis of this framework over the past 10 years. What' s more, the limitations, challenges, and future prospects were proposed, wishing to provide references for the development of pyrazole fused frameworks in the field of medicinal chemistry. Contents.
吡唑骨架与其他骨架的融合创造了一类有吸引力的分子,在药物化学的发展中表现出显著的生物学和化学潜力。在过去的几十年中,已经挖掘和合成了许多具有融合吡唑部分的生物活性分子,其中一些以西地那非为代表已被作为药物上市,融合吡唑化合物的生物学重要性以及化学合成策略,包括基于先导化合物的结构修饰,一直在稳步推进。在这篇综述中,我们关注了融合吡唑的生物学重要性,并强调了过去 10 年中这一框架的合成进展。此外,还提出了局限性、挑战和未来展望,希望为药物化学领域中吡唑融合框架的发展提供参考。内容。