| Literature DB >> 32980515 |
Sameer Agarwal1, Jignesh P Pethani2, Hardik A Shah2, Vismit Vyas2, Santosh Sasane2, Harsh Bhavsar2, Debdutta Bandyopadhyay2, Poonam Giri2, Kasinath Viswanathan2, Mukul R Jain2, Rajiv Sharma3.
Abstract
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 IC50 = 35 nM; IL-18 IC50 = 33 nM) and selective NLRP3 inflammasome inhibitor with excellent pharmacokinetic profile having oral bioavailability of 99% in mice.Entities:
Keywords: Acute respiratory distress syndrome (ARDS); Coronavirus disease 2019 (COVID-19); Inflammation; Interleukin-1β (IL-1β); NLRP3; NLRP3 inflammasome; Sulfonylurea
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Year: 2020 PMID： 32980515 DOI： 10.1016/j.bmcl.2020.127571
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823