2. Academic Validation
  3. Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

  • Eur J Med Chem. 2020 Jan 15:186:111893. doi: 10.1016/j.ejmech.2019.111893.
Zefeng Zhao 1,  Xufen Dai 1,  Chenyang Li 1,  Xiao Wang 1,  Jiale Tian 1,  Ying Feng 1,  Jing Xie 1,  Cong Ma 1,  Zhuang Nie 1,  Peinan Fan 1,  Mingcheng Qian 2,  Xirui He 3,  Shaoping Wu 4,  Yongmin Zhang 5,  Xiaohui Zheng 1
Affiliations

Affiliations

  • 1 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.
  • 2 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.
  • 3 Department of Bioengineering, Zhuhai Campus of Zunyi Medical University, Zhuhai, 519041, China.
  • 4 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. Electronic address: [email protected].
  • 5 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; Sorbonne Université, Institut Parisien de Chimie Moléculaire, CNRS UMR 8232, 4 Place Jussieu, 75005, Paris, France.
PMID: 31761383 DOI: 10.1016/j.ejmech.2019.111893
Abstract

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.

Keywords

Anti-inflammatory; Antimicrobial; Antitumor; CNS agents; Derivatives; Pyrazolone.

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