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Journal of Chinese Pharmaceutical Sciences ›› 2018, Vol. 27 ›› Issue (5): 295-306.DOI: 10.5246/jcps.2018.05.031

• Original articles •     Next Articles

Synthesis and biological evaluation of α,β-unsaturated carbonyl compounds targeting the NLRP3 inflammasome

Qiuyun Kong1, Nan Hang2, Chao Zhang1, Shuchun Li1, Zhongjun Li1, Yang Sun2*, Xiangbao Meng1,2*   

  1. 1. State Key Laboratory of Natural and Biomimetic Drugs; Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
    2. State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing 210023, China
  • Received:2018-01-11 Revised:2018-04-17 Online:2018-05-31 Published:2018-05-02
  • Contact: Tel.: +86-010-82801714, E-mail: xbmeng@bjmu.edu.cn; sunyangnju@163.com
  • Supported by:
    The National Natural Science Foundation of China  (Grant No. 81573272).

Abstract:

A series of α,β-unsaturated ketone derivatives were synthesized, and their anti-inflammatory activity toward NLRP3 inflammasome was evaluated in vitro. Several compounds were identified as anti-inflammatory agents, among which compound A21 exhibited potent anti-inflammatory activity in a dose-dependent manner with an IC50 of 0.95 μM. Moreover, a preliminary structure-activity relationship was also summarized.

Key words: a,β-Unsaturated ketone, NLRP3, IL-1β, Anti-inflammatory

CLC Number: 

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