55687-30-4Relevant academic research and scientific papers
Copper-Catalyzed Divergent C-H Functionalization Reaction of Quinoxalin-2(1H)-ones and Alkynes Controlled by N1-Substituents for the Synthesis of (Z)-Enaminones and Furo[2,3-b]quinoxalines
Feng, Qiong,He, Meiqin,Huang, Huabin,Ji, Fanghua,Jiang, Guangbin,Li, Xuan,Nie, Hongsheng,Wang, Shoucai,Xiong, Zhicheng,Yang, Guang
supporting information, p. 1859 - 1864 (2022/03/16)
With control by N1-substituents, the switchable divergent C-H functionalization reaction of quinoxalin-2(1H)-ones is achieved for the synthesis of (Z)-enaminones and furo[2,3-b]quinoxalines using the combination of a copper catalyst and an oxidant. This new protocol features mild reaction conditions, readily available materials, and a broad substrate scope. Gram-scale and mechanistic studies were also investigated. Furthermore, the desired products exhibited excellent antitumor activity against A549, HepG-2, MCF-7, and HeLa cells, which were tested by MTT assay.
Synthesis and biological evaluation of quinoxaline derivatives as specific c-Met kinase inhibitors
Boggu, Pulla Reddy,Jung, Jun Min,Jung, Young Hoon,Kim, In Su,Kim, Seung Chan,Kim, So Young,Kim, Yeon Su,Ma, Sang Ho,Park, Gi Min,Yu, Ha Na
, (2020/05/08)
A series of novel quinoxaline derivatives were synthesized and evaluated for their inhibitory activity against c-Met kinase enzyme. Most of the tested compounds exhibited potent inhibitory activity. All the synthesized quinoxaline compounds were further e
Photocatalytic Giese Addition of 1,4-Dihydroquinoxalin-2-ones to Electron-Poor Alkenes Using Visible Light
Rostoll-Berenguer, Jaume,Blay, Gonzalo,Pedro, José R.,Vila, Carlos
supporting information, p. 8012 - 8017 (2020/11/02)
The visible-light photoredox-catalyzed coupling of 1,4-dihydroquinoxalin-2-ones and Michael acceptors was achieved using Ru(bpy)3Cl2 as the photocatalyst and (PhO)2PO2H as an additive. The optimized reaction conditions provide a good yield for the radical conjugate addition products (44 examples) with a wide range of structurally different Michael acceptors. A gram scale reaction using sunlight irradiation is also described. Furthermore, several transformations were carried out with the Giese addition products.
TYPE II TOPOISOMERASE INHIBITORS AND METHODS OF MAKING AND USING THEREOF
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, (2018/11/22)
Disclosed are Type II Topoisomerase Inhibitors, analogs thereof, pharmaceutical compositions thereof, and methods of making and using these compounds and compositions. Methods of using the disclosed compounds to treat infections, such as MRSA, MDR P. aeruginosa, and other pathogens are also described.
Hepatitis C virus inhibitors
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Page/Page column 613, (2017/01/23)
Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
BIARYL ACETAMIDE COMPOUNDS AND METHODS OF USE THEREOF
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Paragraph 000178, (2015/03/16)
Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.
Α 7 as intranuclear hydroxynicotinic acetylcholine receptor quinuclidines compd.
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Paragraph 0296; 0297, (2018/10/03)
PROBLEM TO BE SOLVED: To provide ligands for the nicotinic α-7 receptor used for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.SOLUTION: The disclosure provides compounds of the specified formula I, including their salts, and compositions and methods using the compounds.
INHIBITORS OF DNA GYRASE FOR THE TREATMENT OF BACTERIAL INFECTIONS
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Page/Page column 35, (2014/05/07)
The present invention relates to compounds which specifically inhibit bacterial DNA Gyrase and can be used for the treatment of respiratory tract infections.
Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II: Broad-spectrum antibacterial agents with reduced hERG activity
Reck, Folkert,Alm, Richard,Brassil, Patrick,Newman, Joseph,Dejonge, Boudewijn,Eyermann, Charles J.,Breault, Gloria,Breen, John,Comita-Prevoir, Janelle,Cronin, Mark,Davis, Hajnalka,Ehmann, David,Galullo, Vincent,Geng, Bolin,Grebe, Tyler,Morningstar, Marshall,Walker, Phil,Hayter, Barry,Fisher, Stewart
, p. 7834 - 7847 (2012/01/06)
Novel non-fluoroquinolone inhibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) are of interest for the development of new antibacterial agents that are not impacted by target-mediated cross-resistance with fluoroquinolones. Aminopiperidines that have a bicyclic aromatic moiety linked through a carbon to an ethyl bridge, such as 1, generally show potent broad-spectrum antibacterial activity, including quinolone-resistant isolates, but suffer from potent hERG inhibition (IC50= 3 M for 1). We now disclose the finding that new analogues of 1 with an N-linked cyclic amide moiety attached to the ethyl bridge, such as 24m, retain the broad-spectrum antibacterial activity of 1 but show significantly less hERG inhibition (IC 50= 31 M for 24m) and higher free fraction than 1. One optimized analogue, compound 24l, showed moderate clearance in the dog and promising efficacy against Staphylococcus aureus in a mouse thigh infection model.
QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
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Page/Page column 89, (2009/10/31)
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
