吡唑酮结构母核在药物化学中的研究进展与展望。

School of Pharmacy, Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Biomedicine Key Laboratory of Shaanxi Province, Northwest University, 229 Taibai Road, Xi'an, 710069, China.

Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, 213164, Jiangsu, China; Laboratory for Medicinal Chemistry, Ghent University, Ottergemsesteenweg 460, B-9000, Ghent, Belgium.

Eur J Med Chem. 2020 Jan 15;186:111893. doi: 10.1016/j.ejmech.2019.111893. Epub 2019 Nov 16.

The pyrazolone structural motif is a critical element of drugs aimed at different biological end-points. Medicinal chemistry researches have synthesized drug-like pyrazolone candidates with several medicinal features including antimicrobial, antitumor, CNS (central nervous system) effect, anti-inflammatory activities and so on. Meanwhile, SAR (Structure-Activity Relationship) investigations have drawn attentions among medicinal chemists, along with a plenty of analogues have been derived for multiple targets. In this review, we comprehensively summarize the biological activity and SAR for pyrazolone analogues, wishing to give an overall retrospect and prospect on the pyrazolone derivatives.

吡唑酮结构基序是针对不同生物靶点的药物的关键组成部分。药物化学研究已经合成了具有多种药物特性的类药性吡唑酮候选物，包括抗菌、抗肿瘤、中枢神经系统 (CNS) 效应、抗炎活性等。同时，SAR（构效关系）研究引起了药物化学家的关注，并且已经衍生出了针对多种靶标的大量类似物。在这篇综述中，我们全面总结了吡唑酮类似物的生物学活性和 SAR，希望对吡唑酮衍生物进行全面的回顾和展望。