Synthesis and biological evaluation of novel pyrazoline derivatives as potent anti-inflammatory agents. Issue 11 (1st June 2015)

• Record Type: Journal Article
• Authors: He, Jiqiang; Ma, Liang; Wei, Zhe; Zhu, Jun; Peng, Fei; Shao, Mingfeng; Lei, Lei; He, Lin; Tang, Minghai; He, Linhong; Wu, Yuzhe; Chen, Lijuan
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 11(2015)
• Page Start: 2429
• Page End: 2433
• Publication Date: 2015-06-01
• Subjects: Anti-inflammation -- Pyrazolines -- NO production -- iNOS -- Paw edema -- Arthritis; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.03.087
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Twenty-eight pyrazoline derivatives, which originated from pyranochalcones, have been synthesized and evaluated for their inhibitory potency on the production of inflammatory mediator nitric oxide (NO) in LPS-stimulated RAW 264.7 cells. Among them, three compounds (1c, 11c, and15c ) exhibited potent inhibitory effects on NO production and iNOS activity superior to positive control Indomethacin, with1c being most efficacious. Furthermore, 1c could suppress the progress of carrageenan-induced hind paw edema at a dosage of 50 mg/kg/day and dose-dependently ameliorate the development of adjuvant-induced arthritis (AIA). Docking study confirmed that1c was an iNOS inhibitor with good binding into the active site of murine iNOS.