1211284-11-5Relevant articles and documents
Discovery of N-Cyano-sulfoximineurea Derivatives as Potent and Orally Bioavailable NLRP3 Inflammasome Inhibitors
Agarwal, Sameer,Sasane, Santosh,Shah, Hardik A.,Pethani, Jignesh P.,Deshmukh, Prashant,Vyas, Vismit,Iyer, Pravin,Bhavsar, Harsh,Viswanathan, Kasinath,Bandyopadhyay, Debdutta,Giri, Poonam,Mahapatra, Jogeswar,Chatterjee, Abhijit,Jain, Mukul R.,Sharma, Rajiv
supporting information, p. 414 - 418 (2020/03/13)
NLRP3 inflammasome mediated release of interleukin-1β (IL-1β) has been implicated in various diseases. In this study, rationally designed mimics of sulfonylurea moiety were investigated as NLRP3 inhibitors. Our results culminated into discovery of series of unprecedented N-cyano sulfoximineurea derivatives as potent NLRP3 inflammasome inhibitors. Compound 15 (IC50 = 7 nM) and analogues were found to be highly potent and selective NLRP3 inflammasome inhibitor with good pharmacokinetic profile. These effects translate in vivo, as 15, 29, and 34 significantly inhibit NLRP3 dependent IL-1β secretion in mice.
BENZOFURANE DERIVATIVES FOR THE TREATMENT OF HEPATITITS C
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Page/Page column 25, (2012/06/30)
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and maybe useful in treating those infected with HCV.
Reactions of oxetan-3-tert-butylsulfinimine for the preparation of substituted 3-aminooxetanes
Hamzik, Philip J.,Brubaker, Jason D.
supporting information; experimental part, p. 1116 - 1119 (2010/06/11)
(Figure Presented) The oxetane ring Is useful In drug discovery as a bioisostere for both the geminal dimethyl group and the carbonyl group. A convenient, straightforward approach to access structurally diverse 3-aminooxetanes through the reactivity of oxetan-3-tert-butylsulfinimine and the corresponding sulfinylaziridine Is described.