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

doi:10.5246/jcps.2018.05.031

Abstract

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:

R916

Supporting:

Qiuyun Kong, Nan Hang, Chao Zhang, Shuchun Li, Zhongjun Li, Yang Sun, Xiangbao Meng. Synthesis and biological evaluation of α,β-unsaturated carbonyl compounds targeting the NLRP3 inflammasome[J]. Journal of Chinese Pharmaceutical Sciences, 2018, 27(5): 295-306.

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