52206-05-0Relevant articles and documents
POLYCYCLIC COMPOUNDS AS ROR-GAMMA MODULATORS
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Page/Page column 39, (2018/02/27)
The present invention provides compounds which are modulators of RORγ and their use for the treatment of diseases or conditions mediated by RORγ. Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them.
Enamino-oxindole HIV protease inhibitors
Eissenstat, Michael,Guerassina, Tanya,Gulnik, Sergei,Afonina, Elena,Silva, Abelardo M.,Ludtke, Douglas,Yokoe, Hiroko,Yu, Betty,Erickson, John
, p. 5078 - 5083 (2012/09/07)
We have designed and synthesized a series of HIV protease inhibitors (PIs) with enamino-oxindole substituents optimized to interact with the S2′ subsite of the HIV protease binding pocket. Several of these inhibitors have sub-nanomolar Ki and antiviral IC50 in the low nM range against WT HIV and against a panel of multi-drug resistant (MDR) strains.
Identification of inhibitors of NOD1-induced nuclear factor-κB activation
Khan, Pasha M.,Correa, Ricardo G.,Divlianska, Daniela B.,Peddibhotla, Satyamaheshwar,Sessions, E. Hampton,Magnuson, Gavin,Brown, Brock,Suyama, Eigo,Yuan, Hongbin,Mangravita-Novo, Arianna,Vicchiarelli, Michael,Su, Ying,Vasile, Stefan,Smith, Layton H.,Diaz, Paul W.,Reed, John C.,Roth, Gregory P.
experimental part, p. 780 - 785 (2011/12/02)
NOD1 (nucleotide-binding oligomerization domain 1) protein is a member of the NLR (NACHT and leucine rich repeat domain containing proteins) protein family, which plays a key role in innate immunity as a sensor of specific microbial components derived from bacterial peptidoglycans and induction of inflammatory responses. Mutations in NOD proteins have been associated with various inflammatory diseases that affect NF-κB (nuclear factor κB) activity, a major signaling pathway involved in apoptosis, inflammation, and immune response. A luciferase-based reporter gene assay was utilized in a high-throughput screening program conducted under the NIH-sponsored Molecular Libraries Probe Production Center Network program to identify the active scaffolds. Herein, we report the chemical synthesis, structure-activity relationship studies, downstream counterscreens, secondary assay data, and pharmacological profiling of the 2-aminobenzimidazole lead (compound 1c, ML130) as a potent and selective inhibitor of NOD1-induced NF-κB activation.