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Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Bioorg+Med+Chem+Lett 2020 ; 30 (21): 127571 Nephropedia Template TP
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Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor #MMPMID32980515
Bioorg Med Chem Lett 2020[Nov]; 30 (21): 127571 PMID32980515show ga
NLRP3 inflammasome mediated release of interleukin-1beta (IL-1beta) 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-1beta 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.