Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 30, Issue 7, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127021
Keywords
NLRP3; Thiazolidinones; Structure-activity relationship (SAR)
Categories
Funding
- Ministry of Science and Technology [2017YFA0504504, 2016YFA0502001]
- National Natural Science Foundation of China [81661138005, 81422045, 81603131, 91853203]
- Fundamental Research Funds for the Central Universities of China [20720190101, 20720170067]
- Program of Introducing Talents of Discipline to Universities (111 Project) [B06016]
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Aberrant activation of NLRP3 inflammasome is present in a subset of acute and chronic inflammatory diseases. The NLRP3 inflammasome has been recognized as an attractive therapeutic target for developing novel and specific anti-inflammatory inhibitors. Cellular structure-activity relationship-guided optimization resulted in the identification of 4-oxo-2-thioxo-thiazolidinone derivative 9 as a selective and direct small-molecule inhibitor of NLRP3 with IC50 of 2.4 mu M, possessing favorable ex vivo and in vivo pharmacokinetic properties. Compound 9 may represent a lead for the development of anti-inflammatory therapeutics for treating NLRP3-driven diseases.
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