1204-21-3Relevant articles and documents
Intramolecular weak hydrogen bonds in substituted 4-arylthiazoles
Sanchez-Viesca,Berros, Martha,Gomez
, p. 165 - 170 (2003)
We have synthesized new polysubstituted 4-arylthiazoles with a substitution pattern able to form intramolecular weak hydrogen bonds as secondary structure, and besides, displaying in the aromatic region of their 1H-NMR spectra an ABX spin system and only one singlet (the thiazolic proton), thus permitting us to make doubtless assignments. These results confirmed previous assignments made by us in other thiazole-derivatives prepared by the first time. The spectroscopic data (IR, 1H-NMR and MS) of these thiazoles, as well as of the required intermediates, are discussed.
Mutant type IDH inhibitors, preparation method thereof, and pharmaceutical composition containg the same as an active ingredient
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Paragraph 0863-0868, (2021/05/18)
The present invention is a mutated IDH1 inhibitor. The present invention relates to a compound represented by chemical formula 1, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof according to the present invention, which has excellent inhibitory activity against mutated IDH1 and can reduce intracellular tumor-induced metabolite (2-HG), and a health functional food composition for preventing or IDH1 treating cancer, comprising the same as an active ingredient.
Nucleus-independent chemical shift (NICS) as a criterion for the design of new antifungal benzofuranones
González-Chávez, Marco Martín,González-Chávez, Rodolfo,Méndez, Francisco,Martínez, Roberto,Ni?o-Moreno, Perla Del Carmen,Ojeda-Fuentes, Luis Enrique,Richaud, Arlette,Zerme?o-Macías, María de los ángeles
, (2021/08/30)
The assertion made by Wu et al. that aromaticity may have considerable implications for molecular design motivated us to use nucleus-independent chemical shifts (NICS) as an aromaticity criterion to evaluate the antifungal activity of two series of indol-4-ones. A linear regression analysis of NICS and antifungal activity showed that both tested variables were significantly related (p –1 for Candida glabrata, Candida krusei and Candida guilliermondii with compounds 15-32, 15-15 and 15-1. The MIC for filamentous fungi was 1.95 μg·mL–1 for Aspergillus niger for compounds 15-1, 15-33 and 15-34. The results obtained support the use of NICS in the molecular design of compounds with antifungal activity.
One-Pot Preparation of Aromatic Amides, 4-Arylthiazoles, and 4-Arylimidazoles from Arenes
Yamamoto, Takahiro,Togo, Hideo
, p. 4187 - 4196 (2018/08/21)
Simple treatment of arenes with α-bromoacetyl chloride and AlCl3, followed by the reaction with molecular iodine and aq. NH3, thioamides, or amidines gave the corresponding primary aromatic amides, 4-arylthiazoles, or 4-arylimidazoles in good yields, respectively. Aryl α-bromomethyl ketones are the key intermediates in those reactions. Primary aromatic amides were formed from arenes through the reaction of aryl α-bromomethyl ketones with molecular iodine and aq. NH3, and 4-arylthiazoles and 4-arylimidazoles were formed from arenes through the reactions of aryl α-bromomethyl ketones with thioamides and amidines, respectively, in one pot under transition-metal-free conditions.