2. Academic Validation
  3. Synthesis and biological evaluation of novel pyrazoline derivatives as potent anti-inflammatory agents

Synthesis and biological evaluation of novel pyrazoline derivatives as potent anti-inflammatory agents

  • Bioorg Med Chem Lett. 2015 Jun 1;25(11):2429-33. doi: 10.1016/j.bmcl.2015.03.087.
Jiqiang He 1,  Liang Ma 1,  Zhe Wei 1,  Jun Zhu 1,  Fei Peng 1,  Mingfeng Shao 1,  Lei Lei 1,  Lin He 1,  Minghai Tang 1,  Linhong He 1,  Yuzhe Wu 2,  Lijuan Chen 3
Affiliations

Affiliations

  • 1 State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu 610041, China.
  • 2 Chemistry College, Sichuan University, Chengdu, Sichuan 610064, China.
  • 3 State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu 610041, China. Electronic address: chenlijuan125@163.com.
PMID: 25881822 DOI: 10.1016/j.bmcl.2015.03.087
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, and 15c) exhibited potent inhibitory effects on NO production and iNOS activity superior to positive control Indomethacin, with 1c 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 that 1c was an iNOS Inhibitor with good binding into the active site of murine iNOS.

Keywords

Anti-inflammation; Arthritis; NO production; Paw edema; Pyrazolines; iNOS.

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