- Nitrohydroxyquinoline derivative and preparation method and application thereof
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The invention discloses a nitrohydroxyquinoline derivative and a preparation method and application thereof. Specifically, the invention discloses a compound shown as a general formula (I), a preparation method of the compound, a pharmaceutical composition containing the compound, and an application of the compound in treatment on infectious diseases or cancers. The compound disclosed by the invention has different anti-tumor activities and can be developed into a medicine for treating tumors. The definition of each group in the general formula (I) is the same as that in the specification.
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Paragraph 0234-0237
(2020/12/05)
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- Optimization of 8-Hydroxyquinolines as Inhibitors of Catechol O-Methyltransferase
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A series of 8-hydroxy quinolines were identified as potent inhibitors of catechol O-methyltransferase (COMT) with selectivity for the membrane-bound form of the enzyme. Small substituents at the 7-position of the quinoline were found to increase metabolic stability without sacrificing potency. Compounds with good pharmacokinetics and brain penetration were identified and demonstrated in vivo modulation of dopamine metabolites in the brain. An X-ray cocrystal structure of compound 21 in the S-COMT active site shows chelation of the active site magnesium similar to catechol-based inhibitors. These compounds should prove useful for treatment of many neurological and psychiatric conditions associated with compromised cortical dopamine signaling.
- Buchler, Ingrid,Akuma, Daniel,Au, Vinh,Carr, Gregory,De León, Pablo,Depasquale, Michael,Ernst, Glen,Huang, Yifang,Kimos, Martha,Kolobova, Anna,Poslusney, Michael,Wei, Huijun,Swinnen, Dominique,Montel, Florian,Moureau, Florence,Jigorel, Emilie,Schulze, Monika-Sarah E. D.,Wood, Martyn,Barrow, James C.
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p. 9647 - 9665
(2018/11/23)
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- COMT INHIBITING METHODS AND COMPOSITIONS
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The present inventions include a method of inhibiting COMT enzyme in a subject as well as compounds of formula I, or a pharmaceutically acceptable salt thereof, that are useful in the treatment of various disorders mediated by COMT, including Parkinson's disease and/or schizophrenia.
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Paragraph 0276
(2016/08/23)
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- Quinoline synthesis by improved Skraup-Doebner-Von Miller reactions utilizing acrolein diethyl acetal
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A robust synthetic method has been developed as an improvement to the venerable Skraup-Doebner-Von Miller reaction providing access to various quinoline products. The straightforward procedure utilizes acrolein diethyl acetal as a three-carbon annulation partner with aniline substrates in a monophasic, organic solvent-free reaction medium. Differentially substituted aniline precursors were found to be compatible with the reaction conditions and the corresponding quinoline products are isolated in moderate to good yields.
- Ramann, Ginelle A.,Cowen, Bryan J.
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supporting information
p. 6436 - 6439
(2015/11/16)
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- NEUROPROTECTIVE AND NEURO-RESTORATIVE IRON CHELATORS AND MONOAMINE OXIDASE INHIBITORS AND USES THEREOF
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8-Hydroxy-quinoline derivatives and 8-ethers, 8-esters, 8-carbonates, 8-acyloxymethyl, 8- phosphates, (phosphoryloxy)methyl, and 8-carbamates derivatives thereof are described that exhibit iron chelation, neuroprotective, neurorestorative, apoptotic and/or selective MAO-AB inhibitory activities.
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Page/Page column 40-41
(2012/03/09)
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- Fluorinated Alq3 derivatives with tunable optical properties
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This communication reports that not only the emission colour but also the photoluminescence quantum yield of Alq3 can be tuned by introducing fluorine atoms at different positions; with fluorination at C-5 the emission is red-shifted with a tremendously decreased intensity, fluorination at C-6 causes a blue-shift with a significantly increased intensity, and fluorination at C-7 has a minor effect on both the colour and intensity of Alq3's emission. The Royal Society of Chemistry 2006.
- Shi, Yue-Wen,Shi, Min-Min,Huang, Jia-Chi,Chen, Hong-Zheng,Wang, Mang,Liu, Xiao-Dong,Ma, Yu-Guang,Xu, Hai,Yang, Bing
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p. 1941 - 1943
(2008/03/13)
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