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香豆素-吡唑骨架的合成与功能化:最新进展、挑战与机遇。

Synthesis and Functionalization of Coumarin-Pyrazole Scaffold: Recent Development, Challenges, and Opportunities.

机构信息

Organic Chemistry Research Centre, Department of Chemistry, K.T.H.M. College, Nashik-422002, India.

Department of Chemistry, School of Chemical and Life Sciences, Jamia Hamdard, New Delhi-062, India.

出版信息

Curr Org Synth. 2021 Oct 26;18(7):685-710. doi: 10.2174/1570179418666210301122322.

Abstract

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.

摘要

杂环是 DNA 和 RNA 的主要结构基序,在新陈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性质。香豆素和吡唑骨架存在于许多商业药物分子和天然产物中。本文综述了香豆素-吡唑杂环的合成和功能化方面的进展。还讨论了杂环可能的反应部位、功能化以及将吡唑药效团单元纳入合成的机制途径。一些合成和生物学研究表明,香豆素-吡唑部分的结合是发现药物发现中先导化合物的突出结构基序。

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