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 = 35 nM; IL-18 IC = 33 nM) and selective NLRP3 inflammasome inhibitor with excellent pharmacokinetic profile having oral bioavailability of 99% in mice.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7834599 | PMC |
| http://dx.doi.org/10.1016/j.bmcl.2020.127571 | DOI Listing |
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