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Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor

Authors
  • Agarwal, Sameer
  • Pethani, Jignesh P.
  • Shah, Hardik A.
  • Vyas, Vismit
  • Sasane, Santosh
  • Bhavsar, Harsh
  • Bandyopadhyay, Debdutta
  • Giri, Poonam
  • Viswanathan, Kasinath
  • Jain, Mukul R.
  • Sharma, Rajiv
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Sep 24, 2020
Volume
30
Issue
21
Pages
127571–127571
Identifiers
DOI: 10.1016/j.bmcl.2020.127571
PMID: 32980515
PMCID: PMC7834599
Source
PubMed Central
Keywords
Disciplines
  • Article
License
Unknown

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.

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