341-92-4Relevant articles and documents
Toll-like receptor-7 small molecule inhibitor and preparation method thereof
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Paragraph 0130-0132, (2021/02/24)
The invention belongs to the field of chemical small molecules, and particularly relates to a Toll-like receptor-7 small molecule inhibitor. The invention provides the Toll-like receptor-7 small molecule inhibitor, which takes a co-inhibitor of TLR7 and TLR8 obtained by screening as a research object, realizes selective regulation and control of TLR7 and TLR8 through the research on the structureoptimization and structure-activity relationship (SAR) of a parent compound, and further develops a high-efficiency, non-toxic and specific small molecule inhibitor with certain selectivity on TLR 7.The TLR7 small molecule inhibitor has a certain effect and potential medicinal value in autoimmune diseases (systemic lupus erythematosus).
NH+ - F hydrogen bonding in a fluorinated "Proton Sponge" derivative: Integration of solution, solid-state, gas-phase, and computational studies
Scerba, Michael T.,Leavitt, Christopher M.,Diener, Matthew E.,De Blase, Andrew F.,Guasco, Timothy L.,Siegler, Maxime A.,Bair, Nathaniel,Johnson, Mark A.,Lectka, Thomas
scheme or table, p. 7975 - 7984 (2011/12/01)
We report detailed studies on the characterization of an intramolecular NH - F hydrogen bond formed within a fluorinated "proton sponge" derivative. An ammonium ion, generated from 8-fluoro-N,N-dimethylnaphthalen-1- amine, serves as a charged hydrogen bond donor to a covalently bound fluorine appropriately positioned on the naphthalene skeleton. Potentiometric titrations of various N,N-dimethylnaphthalen-1-amines demonstrate a significant increase in basicity when hydrogen bonding is possible. X-ray crystallography reveals that NH - F hydrogen bonding in protonated 8-fluoro-N,N-di-methylnaphthalen-1-amine is heavily influenced by ion pairing in the solid state; bifurcated and trifurcated hydrogen bonds are formed depending on the counterion utilized. Compelling evidence of hydrogen bonding in the 8-fluoro-N,N-dimethylnaphthyl-1- ammonium cation is provided by gas-phase cryogenic vibrational photodissociation spectroscopy. Solution-phase infrared spectroscopy provides complementary results, and the frequencies of the N - H stretching mode in both phases are in excellent agreement with the computed vibrational spectra. NMR analysis of protonated 8-fluoro-N,N-dimethylnaphthalen-1-amine demonstrates significant H - F coupling between the N - H hydrogen and fluorine that cannot be attributed to long-range, through-bond interactions; the couplings correlate favorably with calculated values. The results obtained from these experiments are congruent with the formation of an NH - F hydrogen bond upon protonation of 8-fluoro-N,N-dimethylnaphthalen-1-amine.
1,4-Disubstituted benzo-fused urea compounds
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, (2008/06/13)
Disclosed are compounds of the formulas (I) and (II) shown below which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds. wherein G, X, A and Q are described herein.