Screening of chalcone analogs with anti-depressant, anti-inflammatory, analgesic, and COX-2-inhibiting effects. Issue 11 (1st June 2020)

• Record Type: Journal Article
• Authors: Huang, Zhe-Hao; Yin, Li-Quan; Guan, Li-Ping; Li, Zhao-Hui; Tan, Cheng
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 30:Issue 11(2020)
• Publication Date: 2020-06-01
• Subjects: Quinoline-chalcone -- Anti-depressant -- Anti-inflammatory -- Analgesic -- Neurotransmitters -- COX-2-inhibitory; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2020.127173
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A group of 2-methyl-4-phenylquinoline-chalcone analogs (2a –2x ) was synthesized and investigated for anti-depressant, anti-inflammatory, and analgesic effects as cyclooxygenase-2 inhibitors. Pharmacological experiments identified 24 analogs that exhibited anti-depressant, anti-inflammatory, and analgesic activities. In particular, compounds 2c, 2k, and 2w markedly shortened immobility times and exhibited the most anti-depressant activity. In addition, the mechanisms of action of the analogs 2c, 2k, and 2w were likely related to increased serotonin levels in the central nervous system. Compounds 2c, 2k, and 2w displayed reasonable cyclooxygenase-2 inhibitory effects (IC50 values from 0.21 to 0.29 µmol/L) similar to celecoxib (IC50 : 0.19 µmol/L) in vitro . A molecular docking study of compound 2k also was conducted.