159657-34-8Relevant academic research and scientific papers
Synthesis, characterization and quantum-chemical calculations of novel series of pyridones, quinazolinones and pyrazoles heterocyclic compounds
Salem,Helal,Eldebss, Taha M. A.,Abd-Elaziz,El-Sherif,Mohamed
, p. 1693 - 1707 (2015)
This paper presents a combined synthesis and computational study of novel series of pyridones, quinazolinones and pyrazoles heterocyclic compounds that were characterized by elemental analyses and spectral dada. Michael addition of substituted-2-methoxyca
Structure of the imine 4-hydroxy-2-quinoline ketone compound, and its preparation and use
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Paragraph 0073; 0074, (2016/10/10)
The invention relates to 4-hydroxy-2-quinolinone compounds containing an imine structure, and preparation and an application thereof. A general formula is represented as the formula (I), wherein meanings of groups in the formula are defined in the specification. The compounds represented by the general formula (I) have quite good herbicidal and fungicidal activities and are widely applied in prevention and treatment of weeds and pathogenic bacteria of crops.
Synthesis, biological evaluation and molecular modeling of novel series of pyridine derivatives as anticancer, anti-inflammatory and analgesic agents
Helal,El-Awdan,Salem,Abd-Elaziz,Moahamed,El-Sherif,Mohamed
, p. 764 - 773 (2014/09/29)
This paper presents a combined synthesis; characterization, computational and biological activity studies of novel series of pyridines heterocyclic compounds. The compounds have been characterized by elemental analyses and spectral like IR, 1H NMR, 13C NMR and MS studies. Michael addition of substituted-2-methoxycarbonylacetanilide 2a,b on the α-substituted cinnamonitriles 3a-d gave the corresponding 2-pyridone derivatives 5-10. Structures of the titled compounds cited in this article were elucidated by spectrometric data (IR, 1H NMR, 13C NMR and MS). The molecular modeling of the synthesized compounds has been drawn and their molecular parameters were calculated. Also, valuable information is obtained from the calculation of molecular parameters including electronegativity, net dipole moment of the compounds, total energy, electronic energy, binding energy, HOMO and LUMO energy. Various in vitro antitumor as well as in vivo anti-inflammatory and analgesic activities of the synthesized compounds were investigated. Evaluation of anti-inflammatory activity of test compounds was performed using carrageenan induced paw edema in rats. All the tested compounds showed moderate to good activity. The SAR results indicate that all compounds showed moderate to good activity, among these 7 and 10 compounds having -N(CH3)2 group are most effective.
Ethyl Esters of Malonanilic Acids. Synthesis and Pyrolysis
Ukrainets, Igor V.,Bezugly, Peter A.,Treskach, Vladimir I.,Taran, Svetlana G.,Gorokhova, Olga V.
, p. 10331 - 10338 (2007/10/02)
The pyrolysis under 170-220 deg C or boiling in DMF of malonanilic acids ethyl esters (2) is accompanied by formation of malonic acids symmetric dianilides (7) with high yields.A possible mechanism for this transformation has been suggested.
3-Acyl-4-hydroxyquinolin-2(1H)-ones. Systemically Active Anticonvulsants Acting by Antagonism at the Glycine Site of the N-Methyl-D-Aspartate Receptor Complex
Rowley, Michael,Leeson, Paul D.,Stevenson, Graeme I.,Moseley, Angela M.,Stansfield, Ian,et al.
, p. 3386 - 3396 (2007/10/02)
Most full antagonists at the glycine site of the NMDA receptor contain a carboxylic acid, which we believe to be detrimental to penetration of the blood-brain barrier.By consideration of a pharmacophore, novel antagonists at this site have been designed in which the anionic functionality is a vinylogous acid, in the form of a 4-hydroxyquinolin-2(1H)-one.In this series, a 3-substituent is necessary for binding, and correct manipulation of this group leads to compounds such as the 3-(3-hydroxyphenyl)propargyl ester 24 (L-701,273), with an IC50 for displacement of -L-689,560 binding of 0.17 μM and Kb against NMDA in the cortical slice of 1.39 μM.Compounds were tested for their ability to prevent audiogenic seizure in DBA/2 mice; the most potent compound in this series is the cyclopropyl ketone 42 (L-701,252), with an ED50 of 4.1 mg/kg ip.A model is proposed for binding to the glycine site, in which an important interaction is of a putative receptor cation with the ?-system of the 3-substituent.
