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吡唑啉及相关衍生物的合成方法、生物活性及构效关系。

Synthetic Approaches, Biological Activities, and Structure-Activity Relationship of Pyrazolines and Related Derivatives.

机构信息

Department of Pharmaceutical Chemistry, Noida Institute of Engineering and Technology (Pharmacy Institute), Greater Noida, India.

出版信息

Top Curr Chem (Cham). 2023 Apr 8;381(3):12. doi: 10.1007/s41061-023-00422-z.

Abstract

It has been established that pyrazolines and their analogs are pharmacologically active scaffolds. The pyrazoline moiety is present in several marketed molecules with a wide range of uses, which has established its importance in pharmaceutical and agricultural sectors, as well as in industry. Due to its broad-spectrum utility, scientists are continuously captivated by pyrazolines and their derivatives to study their chemistry. Pyrazolines or their analogs can be prepared by several synthesis strategies, and the focus will always be on new greener and more economical ways for their synthesis. Among these methods, chalcones, hydrazines, diazo compounds, and hydrazones are most commonly applied under different reaction conditions for the synthesis of pyrazoline and its analogs. However, there is scope for other molecules such as Huisgen zwitterions, different metal catalysts, and nitrile imine to be used as starting reagents. The present article consists of recently reported synthetic protocols, pharmacological activities, and the structure-activity relationship of pyrazoline and its derivatives, which will be very useful to researchers.

摘要

已经证实,吡唑啉及其类似物是具有药理活性的支架。吡唑啉部分存在于多种具有广泛用途的市售分子中,这使其在制药和农业以及工业领域都具有重要地位。由于其广谱用途,科学家们一直对吡唑啉及其衍生物着迷,以研究它们的化学性质。吡唑啉或其类似物可以通过几种合成策略来制备,而重点始终是寻找新的、更绿色、更经济的合成方法。在这些方法中,查尔酮、肼、重氮化合物和腙最常用于不同的反应条件下合成吡唑啉及其类似物。然而,其他分子如 Huisgen 两性离子、不同的金属催化剂和腈亚胺也可以用作起始试剂。本文包含了最近报道的吡唑啉及其衍生物的合成方案、药理学活性和构效关系,这对研究人员将非常有用。

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