NLRP3 inflammasome mediated release of interleukin-1β (IL-1β) has been implicated in various diseases, including COVID-19. In this study, rationally designed alkenyl sulfonylurea derivatives were identified as novel, potent and orally bioavailable NLRP3 inhibitors. Compound 7 was found to be potent (IL-1β IC_{50} = 35 nM; IL-18 IC_{50} = 33 nM) and selective NLRP3 inflammasome inhibitor with excellent pharmacokinetic profile having oral bioavailability of 99% in mice.
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【저자키워드】 Inflammation, NLRP3 inflammasome, Coronavirus disease 2019 (COVID-19), acute respiratory distress syndrome (ARDS), NLRP3, interleukin-1β (IL-1β), Sulfonylurea.,
【저자키워드】 Inflammation, NLRP3 inflammasome, Coronavirus disease 2019 (COVID-19), acute respiratory distress syndrome (ARDS), NLRP3, interleukin-1β (IL-1β), Sulfonylurea.,