99433-28-0Relevant articles and documents
Reactivity of substrates with multiple competitive reactive sites toward NBS under neat reaction conditions promoted by visible light
Grjol, Bla?,Jereb, Marjan
, p. 5235 - 5248 (2021/06/07)
Regioselectivity of visible-light-induced transformations of a range of (hetero)aryl alkyl-substituted ketones bearing several competitive reactive sites (α-carbonyl, benzyl and aromatic ring) with N-bromosuccinimide (NBS) was studied under solvent-free reaction conditions (SFRC) and in the absence of inert-gas atmosphere, radical initiators and catalysts. An 8-W energy-saving household lamp was used for irradiation. Heterogeneous reaction conditions were dealt with throughout the study. All substrates were mono- or dibrominated at the α-carbonyl position, and additionally, some benzylic or aromatic bromination was observed in substrates with benzylic carbon atoms or electron-donating methoxy groups, respectively. Surprisingly, ipso-substitution of the acyl group with a bromine atom took place with (4-methoxynaphthyl) alkyl ketones. While the addition of the radical scavenger TEMPO (2,2,6,6-tetramethylpiperidin-1-yloxy) decreased the extent of α- and ring bromination, it completely suppressed the benzylic bromination and α,α-dibromination with NBS under SFRC.
1-phenyl-2-phenylaminoethyl ketone derivative and medical application
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Paragraph 0131; 0132, (2020/04/17)
The invention belongs to the field of pharmaceutical chemicals, and relates to a micromolecular inhibitor of polymyxin drug-resistant protein MCR-1 and application thereof. The invention relates to acompound shown as a formula I, a pharmaceutically accept
Discovery of novel potent GPR40 agonists containing imidazo[1,2-a]pyridine core as antidiabetic agents
Ye, Zhiwen,Liu, Chunxia,Zou, Feng,Cai, Yan,Chen, Bin,Zou, Yuxing,Mo, Jiaxian,Han, Ting,Huang, Wenlong,Qiu, Qianqian,Qian, Hai
, (2020/06/19)
Free fatty acid receptor 1 (FFA1 or GPR40) has been studied for many years as a target for the treatment of type 2 diabetes mellitus. In order to increase potency and reduce hepatotoxicity, a series of novel compounds containing imidazo[1,2-a]pyridine sca
Design, synthesis and biological evaluation of 1-Phenyl-2-(phenylamino) Ethanone Derivatives as Novel MCR-1 Inhibitors
Lan, Xiu-juan,Yan, Hai-tao,Lin, Feng,Hou, Shi,Li, Chen-chen,Wang, Guang-shu,Sun, Wei,Xiao, Jun-hai,Li, Song
supporting information, (2019/08/07)
Polymyxins are considered to be the last-line antibiotics that are used to treat infections caused by multidrug-resistant (MDR) gram-negative bacteria; however, the plasmid-mediated transferable colistin resistance gene (mcr-1) has rendered polymyxins ine
2-AMINO-1,3,4-THIADIAZINE AND 2-AMINO-1,3,4-OXADIAZINE BASED ANTIFUNGAL AGENTS
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Page/Page column 48, (2017/02/09)
The invention provides a compound which is a diazine of formula (I) or a tautomer thereof, or a pharmaceutically acceptable salt thereof, for use as an antifungal agent: (I) wherein X, N', C', A and E are as defined herein. The invention also provides a compound of Formula (I) as defined herein.
Method forsynthesizing ketone by oxidation of alkene under catalysis of iron
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Paragraph 0034; 0035; 0036, (2017/07/23)
The invention discloses a method for synthesizing ketoneby oxidation of alkene under catalysis of iron, and belongs to the field of catalyzed synthesis technologies and fine chemical synthesis. According to the specific method, air or oxygen is taken as an oxidizing agent under the acceleration action ofhydrosilaneand a ketone compound is synthesized byoxidation of alkene under catalysis of iron. The method has the advantages that the catalyst is wide in source, cheap and environment-friendly; the oxidant is wide in source and cheap and does not generate a waste; the reaction conditions are mild, the selectivity is high and the yield is high;a substrate is wide and stable; a functional group of the substrate is good in compatibility and the application range of the substrate is wide; and alkene molecules can be well converted into the ketone. The separation yield of a target product reaches 98% under the optimized reaction conditions.
Antihyperlipidemic morpholine derivatives with antioxidant activity: An investigation of the aromatic substitution
Ladopoulou, Eleni M.,Matralis, Alexios N.,Nikitakis, Anastasios,Kourounakis, Angeliki P.
, p. 7015 - 7023 (2015/11/11)
Drugs affecting more than one target could result in a more efficient treatment of multifactorial diseases as well as fewer safety concerns, compared to a one-drug one-target approach. Within our continued efforts towards the design of multifunctional molecules against atherosclerosis, we hereby report the synthesis of 17 new morpholine derivatives which structurally vary in terms of the aromatic substitution on the morpholine ring. These derivatives simultaneously suppress cholesterol biosynthesis through SQS inhibition (IC50 values of the most active compounds are between 0.7 and 5.5 μM) while exhibiting a significant protection of hepatic microsomal membranes against lipid peroxidation (with IC50 values for the most active compounds being between 73 and 200 μM). Further evaluation of these compounds was accomplished in vivo in an animal model of acute experimental hyperlipidemia, where it was observed that compounds reduced the examined lipidemic parameters (TC, TG and LDL) by 15-80%. In order to examine the mode of binding of these molecules in the active catalytic site of SQS, we also performed docking simulation studies. Our results indicate that some of the new compounds can be considered interesting structures in the search for new multifunctional agents of potential application in atherosclerosis.
2-(4-ARYL-1H-IMIDAZOL-1-YL)ANILINE COMPOUNDS
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Paragraph 0091, (2015/11/27)
The present invention provides compounds that are useful as vaccine adjuvants and/or antitumor agents and methods for producing and using the same. In one particular aspect of the invention, compounds of the invention are of the formula (I) where R1, R2, R3 and Ar1 are those defined herein.
Structure-activity relationship study of 4EGI-1, small molecule eIF4E/eIF4G protein-protein interaction inhibitors
Takrouri, Khuloud,Chen, Ting,Papadopoulos, Evangelos,Sahoo, Rupam,Kabha, Eihab,Chen, Han,Cantel, Sonia,Wagner, Gerhard,Halperin, Jose A.,Aktas, Bertal H.,Chorev, Michael
, p. 361 - 377 (2014/04/17)
Abstract Protein-protein interactions are critical for regulating the activity of translation initiation factors and multitude of other cellular process, and form the largest block of untapped albeit most challenging targets for drug development. 4EGI-1, (E/Z)-2-(2-(4-(3,4-dichlorophenyl)thiazol-2-yl) hydrazono)-3-(2-nitrophenyl)propanoic acid, is a hit compound discovered in a screening campaign of small molecule libraries as an inhibitor of translation initiation factors eIF4E and eIF4G protein-protein interaction; it inhibits translation initiation in vitro and in vivo. A series of 4EGI-1-derived thiazol-2-yl hydrazones have been designed and synthesized in order to delineate the structural latitude and improve its binding affinity to eIF4E, and increase its potency in inhibiting the eIF4E/eIF4G interaction. Probing a wide range of substituents on both phenyl rings comprising the 3-phenylpropionic acid and 4-phenylthiazolidine moieties in the context of both E- and Z-isomers of 4EGI-1 led to analogs with enhanced binding affinity and translation initiation inhibitory activities.
Convenient electrochemical method for the synthesis of-bromo alkyl aryl ketones
Kumar, R. Senthil,Kulangiappar,Kulandainathan, M. Anbu
experimental part, p. 1736 - 1742 (2010/07/05)
An electrochemical procedure for the effective-bromination of alkyl aryl ketones in excellent yield has been reported. The simple experimental procedure, catalyst-free conversion, and excellent yield of monobrominated products are the advantages of this method. Copyright