469898-10-0Relevant academic research and scientific papers
FLUORESCENT SYSTEMS FOR BIOLOGICAL IMAGING AND USES THEREOF
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Page/Page column 26; 28; 36, (2021/02/12)
The invention relates to compounds of formula I, in which Y, Ar1, Ar2, X, R1 and R2 are defined herein, and to their use in a variety of biological imaging techniques and therapeutic methods. In aspects, the invention relates to conjugates comprising the compounds of formula I and their associated uses and therapeutic uses.
Synthesis of 2-substituted 4-arylidene-5(4h)-oxazolones as potential cytotoxic agents in the presence of lemon juice as a biocatalyst
Anand, Krishnan,Jonnalagadda, Sreekantha B.,Katari, Naresh K.,Lakshmi, Chapala V.,Pal, Manojit,Prasad, Malavattu G.
, p. 625 - 634 (2020/01/21)
Background: The oxazolone class of compounds is known to exert a profound effect on malignant cell proliferation, tumor angiogenesis and /or on the established neoplastic vasculature. Additionally, these compounds are generally known to have a low tendenc
Copper nitrate-mediated synthesis of 3-aryl isoxazolines and isoxazoles from olefinic azlactones
Lin, Yifan,Zhang, Ke,Gao, Mingchun,Jiang, Zheyi,Liu, Jiajie,Ma, Yurui,Wang, Haoyu,Tan, Qitao,Xiao, Junjie,Xu, Bin
supporting information, p. 5509 - 5513 (2019/06/14)
A copper nitrate-mediated [2 + 2 + 1] cycloaddition reaction was developed for the expedient synthesis of pharmacologically interesting 3-aryl substituted isoxazolines and isoxazoles through CC bond cleavage. Copper nitrate is employed as a reaction promoter and precursor of nitrile oxides. The given approach features a new mode of cycloaddition from olefinic azlactones, copper nitrate and unsaturated compounds with wide substrate scope, good functional group tolerance and operational simplicity.
Design, synthesis and evaluation of novel phenyl propionamide derivatives as non-nucleoside hepatitis B virus inhibitors
Qiu, Jingying,Gong, Qineng,Gao, Jian,Chen, Wang,Zhang, Yinpeng,Gu, Xiaoke,Tang, Daoquan
, p. 424 - 434 (2018/01/01)
As an ongoing search for potent non-nucleoside anti-HBV agents with novel structures, we described a series of phenyl propionamide derivatives (3a-b, 4a-e, 7a-g, 8a-h and 9a-b) by pharmacophore fusion strategy in the present work. All the compounds exhibited an anti-HBV activity to some extent. Among them, compounds 8d and 9b displayed most potent anti-HBV activity with IC50 values on HBV DNA replication of 0.46 and 0.14 μM, respectively. And the selective index values of 8d and 9b were more than 217.39 and 153.14, suggesting that 8d and 9b exhibited favorable safety profiles. Interestingly, 8d and 9b possessed significantly antiviral activities against lamivudine and entecavir resistant HBV mutants with IC50 values of 0.77 and 0.32 μM. Notably, preliminary anti-HBV action mechanism studies showed that 8d could inhibit intracellular HBV pgRNA and RT activity of the HBV polymerase. Molecular docking studies suggested that compound 8d could fit into the dimer-dimer interface of HBV core protein by hydrophobic interaction. In addition, in silico prediction of physicochemical properties showed that 8d conformed well to the Lipinski's rule of five, suggesting its potential for use as a drug like molecule. Taken together, 8d possessed significantly anti-HBV activity, low toxicity, diverse anti-HBV mechanism and favorable physicochemical properties, and warranted further investigation as a promising non-nucleoside anti-HBV candidate.
Stereoselective Intermolecular [2 + 2] Cycloadditions of Erlenmeyer-Pl?chl Azlactones Using Visible Light Photoredox Catalysis
Marra, Isabellar F. S.,De Almeida, Angelina M.,Silva, Larissa P.,De Castro, Pedro P.,Corrêa, Charlane C.,Amarante, Giovanni Wilson
, p. 15144 - 15154 (2018/12/14)
The first report of the preparation of symmetric and nonsymmetric diaminotruxinic derivatives through the photoredox [2 + 2] cycloadditions of Erlenmeyer azlactones is described, affording the desired compounds in high regio- and diastereocontrol (only head-to-head coupling). Mechanistic studies by DFT suggest that the reaction proceeds through a neutral photocatalytic pathway.
A convenient synthesis of 4-arylidene-2-phenyl-5(4H)-oxazolones under solvent-assisted grinding
Pattarawarapan, Mookda,Jaita, Subin,Phakhodee, Wong
supporting information, p. 3171 - 3174 (2016/07/06)
A facile and effective approach for the synthesis of 4-arylidene-2-phenyl-5(4H)-oxazolones has been developed. Under solvent-assisted grinding in the presence of 2,4,6-trichloro-1,3,5-triazine, catalytic triphenylphosphine, and sodium carbonate, dehydrati
Oxazolone-based photoswitches: Synthesis and properties
Blanco-Lomas, Marina,Funes-Ardoiz, Ignacio,Campos, Pedro J.,Sampedro, Diego
supporting information, p. 6611 - 6618 (2013/11/06)
The synthesis, photophysics and photochemistry of a family of molecular switches inspired by the green fluorescent protein (GFP) chromophore is presented. These compounds can be synthesized in one step and good yields, their photophysical properties may b
Benzylidene-oxazolones as photoswitches: Photochemistry and theoretical calculations
Funes-Ardoiz, Ignacio,Blanco-Lomas, Marina,Campos, Pedro J.,Sampedro, Diego
supporting information, p. 9766 - 9771 (2013/10/22)
The photophysics and photochemistry of a family of compounds proposed as efficient molecular photoswitches is presented. The effect of different light sources, substituents and solvents in the photostationary state has been explored. A detailed mechanisti
Benzylidene-oxazolones as molecular photoswitches
Blanco-Lomas, Marina,Campos, Pedro J.,Sampedro, Diego
supporting information, p. 4334 - 4337 (2012/10/29)
The synthesis and photochemical study of a family of molecular switches inspired by the green fluorescent protein (GFP) chromophore is presented. These compounds can be easily synthesized, and their photophysical properties may be tuned. Due to their effi
Palladium-catalyzed diastereo- and enantioselective formal [3 + 2]-cycloadditions of substituted vinylcyclopropanes
Trost, Barry M.,Morris, Patrick J.,Sprague, Simon J.
supporting information, p. 17823 - 17831,9 (2012/12/12)
We describe a palladium-catalyzed diastereo- and enantioselective formal [3 + 2]-cycloaddition between substituted vinylcyclopropanes and electron-deficient olefins in the form of azlactone- and Meldrums acid alkylidenes to give highly substituted cyclopentane products. By modulation of the electronic properties of the vinylcyclopropane and the electron-deficient olefin, high levels of stereoselectivity were obtained. The remote stereoinduction afforded by the catalyst, distal from the chiral pocket generated by the ligand, is proposed to be the result of a new mechanism invoking the Curtin-Hammett principle.
