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10.1016/j.bmcl.2020.127571

http://scihub22266oqcxt.onion/10.1016/j.bmcl.2020.127571
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32980515!7834599!32980515
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suck abstract from ncbi


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pmid32980515      Bioorg+Med+Chem+Lett 2020 ; 30 (21): 127571
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  • Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor #MMPMID32980515
  • Agarwal S; Pethani JP; Shah HA; Vyas V; Sasane S; Bhavsar H; Bandyopadhyay D; Giri P; Viswanathan K; Jain MR; Sharma R
  • 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.
  • |Administration, Oral[MESH]
  • |Animals[MESH]
  • |Betacoronavirus[MESH]
  • |COVID-19[MESH]
  • |Cell Line, Tumor[MESH]
  • |Coronavirus Infections[MESH]
  • |Cytochrome P-450 CYP2C8 Inhibitors/administration & dosage/chemical synthesis/pharmacokinetics/pharmacology[MESH]
  • |Cytochrome P-450 CYP2C9 Inhibitors/administration & dosage/chemical synthesis/pharmacokinetics/pharmacology[MESH]
  • |Dogs[MESH]
  • |Drug Stability[MESH]
  • |Humans[MESH]
  • |Inflammasomes/*antagonists & inhibitors[MESH]
  • |Interleukin-1beta/antagonists & inhibitors[MESH]
  • |Mice, Inbred C57BL[MESH]
  • |Microsomes, Liver/metabolism[MESH]
  • |Molecular Structure[MESH]
  • |NLR Family, Pyrin Domain-Containing 3 Protein/*antagonists & inhibitors[MESH]
  • |Pandemics[MESH]
  • |Pneumonia, Viral[MESH]
  • |Rats[MESH]
  • |SARS-CoV-2[MESH]
  • |Structure-Activity Relationship[MESH]


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