Relevant bibliographies by topics / 3,4-Dihydro-2(1H)-quinolinone

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  2. Dissertations / Theses
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Academic literature on the topic '3,4-Dihydro-2(1H)-quinolinone'

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Published: 4 June 2021
Last updated: 4 February 2022

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Journal articles on the topic "3,4-Dihydro-2(1H)-quinolinone"

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Wu, Lingang, Yanan Hao, Yuxiu Liu, and Qingmin Wang. "NIS-mediated oxidative arene C(sp2)–H amidation toward 3,4-dihydro-2(1H)-quinolinone, phenanthridone, and N-fused spirolactam derivatives." Organic & Biomolecular Chemistry 17, no. 28 (2019): 6762–70. http://dx.doi.org/10.1039/c9ob01277j.

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A new radical-mediated intramolecular arene C(sp2)–H amidation of 3-phenylpropanamides or [1,1′-biphenyl]-2-carboxamides was developed to prepare a series of 3,4-dihydro-2(1H)-quinolinone and phenanthridone derivatives in moderate to excellent yields (33–94%).
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Meiring, Letitia, Jacobus P. Petzer, and Anél Petzer. "Inhibition of monoamine oxidase by 3,4-dihydro-2(1H)-quinolinone derivatives." Bioorganic & Medicinal Chemistry Letters 23, no. 20 (October 2013): 5498–502. http://dx.doi.org/10.1016/j.bmcl.2013.08.071.

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Tu, Shu-Jiang, Bo Jiang, Xiao-Tong Zhu, and Qiu-Yun Li. "Highly Efficient Synthesis of 3,4-Dihydro-2(1H)-quinolinone Derivatives under Microwave Heating." HETEROCYCLES 85, no. 7 (2012): 1615. http://dx.doi.org/10.3987/com-12-12489.

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Zhao, He, Andrew Thurkauf, Julia Braun, Robin Brodbeck, and Andrzej Kieltyka. "Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives." Bioorganic & Medicinal Chemistry Letters 10, no. 18 (September 2000): 2119–22. http://dx.doi.org/10.1016/s0960-894x(00)00421-2.

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Tsuritani, Takayuki, Yuhei Yamamoto, Masashi Kawasaki, and Toshiaki Mase. "Novel Approach to 3,4-Dihydro-2(1H)-quinolinone Derivatives via Cyclopropane Ring Expansion." Organic Letters 11, no. 5 (March 5, 2009): 1043–45. http://dx.doi.org/10.1021/ol802669r.

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Oshiro, Yasuo, Yoji Sakurai, Seiji Sato, Nobuyuki Kurahashi, Tatsuyoshi Tanaka, Tetsuro Kikuchi, Katsura Tottori, Yasufumi Uwahodo, Takashi Miwa, and Takao Nishi. "3,4-Dihydro-2(1H)-quinolinone as a Novel Antidepressant Drug: Synthesis and Pharmacology of 1-[3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl]-3,4- dihydro-5-methoxy-2(1H)-quinolinone and Its Derivatives." Journal of Medicinal Chemistry 43, no. 2 (January 2000): 177–89. http://dx.doi.org/10.1021/jm980333v.

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Zhu, Xiao-Tong, Qiu-yun Li, Bo Jiang, and Shu-Jiang Tu. "ChemInform Abstract: Highly Efficient Synthesis of 3,4-Dihydro-2(1H)-quinolinone Derivatives under Microwave Heating." ChemInform 43, no. 45 (October 11, 2012): no. http://dx.doi.org/10.1002/chin.201245178.

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Oshiro, Yasuo, Yoji Sakurai, Seiji Sato, Nobuyuki Kurahashi, Tatsuyoshi Tanaka, Tetsuro Kikuchi, Katsura Tottori, Yasufumi Uwahodo, Takashi Miwa, and Takao Nishi. "ChemInform Abstract: 3,4-Dihydro-2(1H)-quinolinone as a Novel Antidepressant Drug: Synthesis and Pharmacology of 1-[3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl] -3,4-dihydro-5-methoxy-2(1H)-quinolinone and Its Derivatives." ChemInform 31, no. 16 (June 9, 2010): no. http://dx.doi.org/10.1002/chin.200016149.

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Sun, Qun, Xiaoming Zhou, and Donald J. Kyle. "Solid-phase synthesis of 3,4-dihydro-2(1H)-quinazolinones and 3,4-dihydro-1H-quinazolin-2-thiones." Tetrahedron Letters 42, no. 25 (June 2001): 4119–21. http://dx.doi.org/10.1016/s0040-4039(01)00691-8.

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Rádl, Stanislav, Viktor Zikán, and František Šmejkal. "Syntheses of some N-carboxymethyl derivatives of 4,9-dihydro-3-methyl-4-oxo-1H-(2H)-pyrazolo[3,4-b]quinoline with antiviral effects." Collection of Czechoslovak Chemical Communications 50, no. 9 (1985): 2010–14. http://dx.doi.org/10.1135/cccc19852010.

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The paper describes the syntheses of 4,9-dihydro-9-carboxymethyl-1,3-dimethyl-4-oxo-1H-pyrazolo[3,4-b]quinoline (Ic), 4,9-dihydro-9-carboxymethyl-2,3-dimethyl-4-oxo-2H-pyrazolo[3,4-b]quinoline (IIc), 4,9-dihydro-1-carboxymethyl-3-methyl-4-oxo-1H-pyrazolo[3,4-b]quinoline (Id), 4,9-dihydro-1-carboxymethyl-3,9-dimethyl-4-oxo-1H-pyrazolo[3,4-b]quinoline (If) and 4,9-dihydro-2-carboxymethyl-3,9-dimethyl-4-oxo-2H-pyrazolo[3,4-b]quinoline (IIf). The compounds were tested in vivo in mice for their efficacy against the virus A2-Hongkong and the encephalomyocarditis virus.
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Dissertations / Theses on the topic "3,4-Dihydro-2(1H)-quinolinone"

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Touzeau, Frédérique. "Syntheses et proprietes pharmacologiques de 2-(4,5-dihydro-1h-2-imidazolyl)-3,4-dihydro-2h-1,4-benzoxazines diversement substituees." Orléans, 1998. http://www.theses.fr/1998ORLE2023.

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L'hypertension arterielle est une pathologie qui concerne plus de 10% de la population adulte. Pour son traitement, il existe toute une gamme de medicaments tres actifs repartis en plusieurs classes distinctes (les diuretiques, les bloquants, les antagonistes calciques, les inhibiteurs de l'enzyme de conversion, les antihypertenseurs centraux). Depuis quelques annees d'autres composes actifs ont ete mis en evidence qui font intervenir de nouveaux recepteurs notamment les recepteurs aux imidazolines. Le but de ce travail est de synthetiser des composes susceptibles d'avoir une activite antihypertensive centrale sans les effets secondaires de produits deja connus, grace a une bonne affinite pour les recepteurs aux imidazolines. Nos premiers travaux ont concerne la synthese de divers analogues de l'idazoxan qui possedent le motif 2,3-dihydro-1,4-benzodioxine. Cette etude a permis de mettre en evidence que pour avoir une bonne affinite pour les recepteurs imidazoliniques, le motif imidazoline etait indispensable. Par la suite, nous nous sommes interesse a la synthese de 3,4-dihydro-2h-1,4-benzoxazines diversement substituees soit par differents groupements alkyles au niveau de l'azote soit par differents groupements (methyle, chloro, methoxy) sur le noyau aromatique. Nous avons egalement considere la substitution en position alpha de l'imidazoline. Les resultats pharmacologiques ont montre que le motif 2,3-dihydro-2h-1,4-benzoxazinique judicieusement substitue permet d'obtenir une bonne affinite pour les recepteurs aux imidazolines et #2 adrenergiques. Nous avons aussi prepare des imidazolines comportant un motif benzoxazinique associe a un troisieme cycle constitue de 5,6 et 7 chainons. Ces composes sont prepares selon deux approches differentes ; l'une faisant intervenir la 7-hydroxyindoline et l'autre le 2,3-dihydro-2h-1,4-benzoxazine-2-carboxylate d'ethyle. Parmi les composes que nous avons synthetises quatre d'entre eux se distinguent par une bonne affinite vis a vis des recepteurs aux imidazolines i#2 et #2 adrenergiques. Ces composes sont aussi actifs in vivo. Ces resultats tres encourageants laissent entrevoir des developpements futurs pour mieux cerner le profil pharmacologique de ces composes.
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Ba, Lalla Aîcha Kirsch Gilbert. "Nouvelles approches vers la synthèse de l'acide 5-(2-oxo-2,3-dihydro-1H-thiéno[3,4-d]imidazol-4-yl) pentanoïque (tétradéhydrobiotine)." [S.l.] : [s.n.], 2007. ftp://ftp.scd.univ-metz.fr/pub/Theses/2007/Ba_Lalla.Aicha.SMZ0745.pdf.

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Ba, Lalla Aïcha. "Nouvelle approche vers la synthèse de l'acide 5-(-2-oxo-2,3-dihydro-1H-thiéno[3,4-d]imidazol-4-yl) pentanoïque (la tétradéhydrobiotine)." Thesis, Metz, 2007. http://www.theses.fr/2007METZ045S/document.

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La biotine ou vitamine H est un coenzyme impliqué dans les processus de transfert de dioxyde de carbone sur diverses molécules naturelles. Sa très grande affinité avec l'avidine ou la streptavidine est couramment exploitée dans le cadre de différentes méthodes d'analyse biochimiques telles que la purification et la détection de protéines. Cependant cette affinité très élevée peut aussi constituer un inconvénient suivant l'utilisation recherchée car la rupture de l'interaction avidine-biotine-protéine d'intérêt implique des conditions de dénaturation drastiques peu compatibles avec l'obtention d’une protéine encore active. La préparation de nouveaux analogues de la biotine présentant une affinité modérée vis-à-vis de l’avidine et de la streptavidine pourrait permettre de faciliter la purification de protéine dans leur état natif. Dans cette optique et en collaboration avec l'équipe de biologistes de notre laboratoire, notre projet est de synthétiser un analogue de la biotine : la 2,3,4,5-tétradéhydrobiotine, puis d'évaluer l'interaction de ce composé avec l’avidine. Dans nos travaux nous avons isolé différents intermédiaires intéressants qui pourront être utilisés dans la synthèse de la tétradéhydrobiotine. Lors de cette étude nous avons également synthétisé de nouveaux thiéno[2,3-d]imidazolones substitués en position 5 au départ de l'hydantoïne
Intracellular biotin is a coenzyme in carbon dioxyde transport. Futhermore because of their high affinity, avidin-biotin or streptavidin-biotin coupling is often used in different biochemical analyses such as protein purification and detection. The high avidin/streptavidin-biotin affinity can also constitute a drawback since proteins require to be denaturated in order to be released, and therefore are often lacking activity. In order to identify pure and active proteins target using this methodology, our aim was to synthesize an analog of biotin: 2,3,4,5-tetradehydrobiotin. We have isolated different key intermediates for the synthesis of tetradehydrobiotin. During this study we also synthesize news thieno[2,3-d]imidazolones starting from hydantoin
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Letellier, Marie-Anne. "Synthèse et évaluation pharmacologique de dérivés des noyaux 4,4-dyméthil-3,4-dihydro-1H-quinoléin-2-one et 1H-pyrrolo[2,3-b]pyridin-2(3H)-one en tant qu'inhibiteurs de la Rho-kinase en vue d'un traitement contre l'hypertension." Tours, 2007. http://www.theses.fr/2007TOUR3803.

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L’hypertension artérielle (HTA) touche dans les pays industrialisés près de 15% de la population adulte. Lorsqu’on ne peut déceler de cause à l’élévation de la pression artérielle dans les vaisseaux, on parle d’HTA essentielle ou primaire. Une contraction normale du muscle lisse, dont le mécanisme fait intervenir la petite protéine G Rho et sa cible Rho-kinase, entraîne le rétrécissement du diamètre des vaisseaux et provoque une élévation de la pression artérielle. Ainsi, des inhibiteurs de Rho-kinase pourraient se révéler utiles dans le traitement de l’hypertension. Les objectifs fixés consistaient en la conception et l’élaboration de nouveaux inhibiteurs de la Rho-kinase en termes de sélectivité, de biodisponibilité et d’originalité structurale. Ainsi, des dérivés des noyaux 4,4-diméthyl-3,4-dihydro-1H-quinoléin-2-one et 1H-pyrrolo[2,3-b]pyridin-2(3H)-one ont été synthétisés et ont fait l’objet d’études pharmacologiques effectuées par les laboratoires SERVIER
Over a billion people are suffering from arterial hypertension, a disease defined by a rise in the blood pressure in the arteries due to the abnormal contraction of the smooth-muscle. The contraction is regulated by the cytosolic calcium concentration to which the Rho/Rho-kinase intracellular pathway is associated. Designing compounds that inhibit the enzyme is of great interest. We have elaborated new potential Rho-kinase inhibitors. Various molecules were synthesized based on the 4,4-dimethyl-3,4-dihydro-1H-quinolin-2-one and the 1H-pyrrolo[2,3-b]pyridin-2(3H)-one chemistry. The new compounds were then studied by our collaborators, les laboratories SERVIER, for their activity on Rho-kinase inhibition
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Meiring, Letitia. "Monoamine oxidase inhibition by novel quinolinones / Letitia Meiring." Thesis, 2014. http://hdl.handle.net/10394/11189.

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Parkinson’s disease (PD) is an age-related neurodegenerative disorder. The degeneration of the neurons of the substantia nigra in the midbrain leads to the loss of dopamine from the striatum, which is responsible for the motor symptoms of PD. In the brain, the enzyme, monoamine oxidase B (MAOB), An analysis of the Lineweaver-Burk plots indicated that 7-(3-bromobenzyloxy)-3,4-dihydro-2(1H)- quinolinone inhibits MAO-B with a Ki value of 2.7 nM. An analysis of the structure-activity relationships for MAO-B inhibition shows that substitution on the C7 position of the 3,4-dihydro- 2(1H)-quinolinone moiety leads to significantly more potent inhibition compared to substitution on C6. In this regard, a benzyloxy substituent on C7 is more favourable than phenylethoxy and phenylpropoxy substitution on this position. In spite of this, C6-substituted 3,4-dihydro-2(1H)-quinolinone with potent MAO-B inhibitory activities were also identified. An analyses of selected properties of the 3,4-dihydro-2(1H)- quinolinones showed that the compounds are highly lipophilic with logP values in the range of 3.03- 4.55. LogP values between 1 and 3 are, however, in the ideal range for bioavailability. The compounds synthesised have logP values higher than 3, which may lead to lower bioavailability. Laboratory data further showed that none of the 3,4-dihydro-2(1H)-quinolinones are highly toxic to cultured cells at the concentrations, 1 μM and 10 μM, tested. For example, the most potent MAO-B inhibitor, 7-(3-bromobenzyloxy)-3,4-dihydro-2(1H)-quinolinone, reduced cell viability to 88.11% and 86.10% at concentrations of 1 μM and 10 μM, respectively. These concentrations are well above its IC50 value for the inhibition of MAO-B. At concentrations required for MAO-B inhibition, the more potent 3,4-dihydro-2(1H)-quinolinones are thus unlikely to be cytotoxic. It may thus be concluded that C7-substituted 3,4-dihydro-2(1H)-quinolinones are promising highly potent and selective MAO-B inhibitors, and thus leads for the therapy of Parkinson’s disease. represents a major catabolic pathway of dopamine. Inhibitors of MAO-B conserve the depleted supply of dopamine and are thus used in the therapy of PD. In the present study, a series of 3,4- dihydro-2(1H)-quinolinone derivatives were synthesized and evaluated as inhibitors of recombinant human MAO-A and MAO-B. These quinolinone derivatives are structurally related to a series of coumarin (1-benzopyran-2-one) derivatives, which has been reported to act as MAO-B inhibitors. C6- and C7-substituted 3,4-dihydro-2(1H)-quinolinone derivatives were synthesized by reacting 6- or 7- hydroxy-3,4-dihydro-2(1H)-quinolinone with an appropriately substituted alkyl bromide in the presence of base. To evaluate the MAO inhibitory properties (IC50 values) of the quinolinone derivatives the recombinant human MAO-A and MAO-B enzymes were used. The reversibility of inhibition of a representative 3,4-dihydro-2(1H)-quinolinone derivative was examined by measuring the recovery of enzyme activity after the dilution of the enzyme-inhibitor complexes, while the mode of MAO inhibition was determined by constructing Lineweaver-Burk plots. To determine the lipophilicity of the 3,4-dihydro-2(1H)-quinolinone derivatives, the logP values were measured. The toxicity of the 3,4-dihydro-2(1H)-quinolinone derivatives towards cultured cells (cytotoxicity) was also measured. The results document that the 3,4-dihydro-2(1H)-quinolinone derivatives are highly potent and selective MAO-B inhibitors with most homologues exhibiting IC50 values in the nanomolar range. The most potent MAO-B inhibitor, 7-(3-bromobenzyloxy)-3,4-dihydro-2(1H)-quinolinone, exhibits an IC50 value of 2.9 nM with a 2750-fold selectivity for MAO-B over the MAO-A isoform. As a MAO-B inhibitor, this compound is approximately equipotent to the most potent coumarin derivative (IC50 = 1.14 nM) reported in literature. Since MAO-B activity could be recovered after dilution of enzyme-inhibitor mixtures, it may be concluded that 7-(3-bromobenzyloxy)-3,4-dihydro-2(1H)- quinolinone is a reversible MAO-B inhibitor. The Lineweaver-Burk plots constructed for the inhibition of MAO-B by 7-(3-bromobenzyloxy)-3,4-dihydro-2(1H)-quinolinone were linear and intersected on the y-axis. These data indicated that this compound also is a competitive MAO-B inhibitor.
MSc (Pharmaceutical Chemistry), North-West University, Potchefstroom Campus, 2014
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Book chapters on the topic "3,4-Dihydro-2(1H)-quinolinone"

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Sanders, Stephan, Kate Snyder, Kara Hume, Christi Carnahan, and Stephan Sanders. "7-[4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydro-2(1H)-quinolinone." In Encyclopedia of Autism Spectrum Disorders, 8. New York, NY: Springer New York, 2013. http://dx.doi.org/10.1007/978-1-4419-1698-3_100031.

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Hirota, E., K. Kuchitsu, T. Steimle, J. Vogt, and N. Vogt. "222 C14H8O6 8b,8c-Dihydro-8b,8c-dimethyl-1H,3H,5H,7H-furo[3'',4'':1',3']cyclopropa[1',2',3':3,4]pentaleno[1,6-cd]pyran-1,3,5,7-tetrone." In Molecules Containing Three or Four Carbon Atoms and Molecules Containing Five or More Carbon Atoms, 409–10. Berlin, Heidelberg: Springer Berlin Heidelberg, 2014. http://dx.doi.org/10.1007/978-3-642-41504-3_353.

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"7-[4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydro-2(1H)-quinolinone." In Encyclopedia of Autism Spectrum Disorders, 9. Cham: Springer International Publishing, 2021. http://dx.doi.org/10.1007/978-3-319-91280-6_300009.

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Conference papers on the topic "3,4-Dihydro-2(1H)-quinolinone"

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Anichina, K. "SYNTHESIS AND ANTINEMATODAL ACTIVITY STUDIES OF SOME FUSED TRIAZINOBENZIMIDAZOLES." In International Trends in Science and Technology. RS Global Sp. z O.O., 2020. http://dx.doi.org/10.31435/rsglobal_conf/30122020/7351.

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4-Aryl-3,4-dihydro[1,3,5]triazino[1,2-a]benzimidazole-2-amines 3a-f were synthesized in the reaction of cyclocondensation between 2-guanidinobenzimidazole and versatilebenzaldehydes. Structures of all prepared compounds were confirmed by IR, 1H NMR spectroscopyand elemental analysis.Antinematodal activity in vitro of the substances was investigated using isolated Trichinella spiralis muscle larvae. The tested triazonobenzimidazoles showed different activity depending on the substituent R in their moleculeas the derivatives substituted with a hydroxyl group demonstrated the best anti-Trichinella spiralis activity in the series.
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