Synthesis and anti-inflammatory evaluation of new chalcone derivatives bearing bispiperazine linker as IL-1β inhibitors
| Autor: | Xiao-Jia Pu, Wei-Lie Xiao, Xi Zheng, Chun-Ping Wan, Xiao-Si Li, Yan-Ling Tang, Xia Zhang, Bei Liu, Ze-Wei Mao, Yan Qi |
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| Rok vydání: | 2019 |
| Předmět: |
Lipopolysaccharides
Chalcone medicine.drug_class Stereochemistry Interleukin-1beta Nitric Oxide 01 natural sciences Biochemistry Anti-inflammatory chemistry.chemical_compound Mice Structure-Activity Relationship Drug Discovery medicine Cytotoxic T cell Animals Cytotoxicity Molecular Biology Piperazine integumentary system Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Chemistry Organic Chemistry Anti-Inflammatory Agents Non-Steroidal In vitro 0104 chemical sciences 010404 medicinal & biomolecular chemistry RAW 264.7 Cells Mice Inbred DBA NLRP3 inflammasome activation Linker |
| Zdroj: | Bioorganic chemistry. 98 |
| ISSN: | 1090-2120 |
| Popis: | In this work, a series of novel chalcone derivatives bearing bispiperazine linker have been synthesized and in vitro anti-inflammatory, cytotoxic activity and anti-inflammatory mechanism have been screened. The results indicated that most bispiperazinochalcone derivatives displayed good inhibition of NO (IC50 40 μM), and selectively inhibited the production of IL-1β via inhibiting NLRP3 inflammasome activation, as promising candidate compounds for the treatment of NLRP3 inflammasome-driven diseases. |
| Databáze: | OpenAIRE |
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