Structure-Stability Relationship of NLRP3 Inflammasome-Inhibiting Sulfonylureas.
ACS Omega
; 7(9): 8158-8162, 2022 Mar 08.
Article
em En
| MEDLINE
| ID: mdl-35284735
ABSTRACT
In recent drug development efforts, particular emphasis has been devoted to the chemical interference with the NLRP3 inflammasome. A series of 12 tailored sulfonylureas was designed, prepared through convergent syntheses with a final sodium hydride-promoted reaction of isocyanates and sulfonamides, and subjected to a systematic, high-performance liquid chromatography-based survey of the chemical stability, a critical issue of sulfonylureas in terms of preparation, storage, and application. NLRP3 binding was determined by surface plasmon resonance spectroscopy. Sulfonylurea 2 was identified to be equipotent and similarly stable compared to the prototypical NLRP3 inhibitor MCC950.
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MEDLINE
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En
Ano de publicação:
2022
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Article