Relevant bibliographies by topics / Quinazoline

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  1. Journal articles
  2. Dissertations / Theses
  3. Books
  4. Book chapters
  5. Conference papers

Academic literature on the topic 'Quinazoline'

Author: Grafiati
Published: 4 June 2021
Last updated: 12 June 2025

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Journal articles on the topic "Quinazoline"

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Abu-Hashem, Ameen. "Synthesis of New Furothiazolo Pyrimido Quinazolinones from Visnagenone or Khellinone and Antimicrobial Activity." Molecules 23, no. 11 (2018): 2793. http://dx.doi.org/10.3390/molecules23112793.

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Substituted-6-methyl-1-thioxo-1,2-dihydro-3H-furo[3,2-g]pyrimido[1,6-a]quinazolin-3-ones (5a,b) were synthesized from condensation of visnagenone (2a) or khellinone (2b) with 6-amino-thiouracil (3) in dimethylformamide or refluxing of (4a) or (4b) in dimethylformamide. Hence, compounds (5a,b) were used as the starting materials for preparing many new heterocyclic compounds such as; furo[3,2-g]pyrimido[1,6-a]quinazoline (6a,b), furo[3,2-g]thiazolo[2′,3′:2,3]pyrimido[1,6-a]quinazolinone (7a,b), substituted-benzylidene-furo[3,2-g]thiazolo[2′,3′:2,3]pyrimido[1,6-a]quinazoline-3,5-dione (8a–f), 3-oxo-furo[3,2-g]pyrimido[1,6-a]quinazoline-pentane-2,4-dione (9a,b), 1-(pyrazole)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (10a,b), 2-(oxo or thioxo)-pyrimidine-furo[3,2-g]pyrimido[1,6-a]quinazolinone (11a–d), 1-(methylthio)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (12a,b), 1-(methyl-sulfonyl)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (13a,b) and 6-methyl-1-((piperazine) or morpholino)-3H-furo[3,2-g]pyrimido[1,6-a]quinazolin-3-one (14a–d). The structures of the prepared compounds were elucidated on the basis of spectral data (IR, 1H-NMR, 13C-NMR, MS) and elemental analysis. Antimicrobial activity was evaluated for the synthesized compounds against Gram-positive, Gram-negative bacteria and fungi. The new compounds, furothiazolo pyrimido quinazolines 8a–f and 11a–d displayed results excellent for growth inhibition of bacteria and fungi.
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Vishwakarma, Lav Kush Kumar, and Varsha Kashaw. "Nanocatalyzed Synthetic Approach for the Quinazolinone and Quinazoline Derivatives: A Review (2015 – Present)." Journal of Drug Delivery and Therapeutics 13, no. 3 (2023): 171–83. http://dx.doi.org/10.22270/jddt.v13i3.5765.

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Due to their diverse chemical reactivities and essential range of biological action, quinazolines and their derivatives rank among the most significant heterocyclic compounds. Quinazoline and quinazolinone scaffolds pharmacological properties have sparked medicinal chemists' interest in creating original medications or drug candidates. The growth of quinazoline hybrid lead compounds and the related heterocycles is summarised in the current review of medicinal chemistry. Additionally, by shedding light on the potential significance of these hybridised pharmacophoric characteristics in the demonstrating a range of pharmacological activities, the review contributes to the acceleration of the drug development process.
 Keywords: Fused Heterocycles, Quinazolinone and Quinazoline Derivatives, Drug Development
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Asif, Mohammad. "Chemical Characteristics, Synthetic Methods, and Biological Potential of Quinazoline and Quinazolinone Derivatives." International Journal of Medicinal Chemistry 2014 (November 13, 2014): 1–27. http://dx.doi.org/10.1155/2014/395637.

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The heterocyclic fused rings quinazoline and quinazolinone have drawn a huge consideration owing to their expanded applications in the field of pharmaceutical chemistry. Quinazoline and quinazolinone are reported for their diversified biological activities and compounds with different substitutions bring together to knowledge of a target with understanding of the molecule types that might interact with the target receptors. Quinazolines and quinazolinones are considered as an important chemical for the synthesis of various physiological significance and pharmacological utilized molecules. Quinazolines and quinazolinone are a large class of biologically active compounds that exhibited broad spectrum of biological activities such as anti-HIV, anticancer, antifungal, antibacterial, antimutagenic, anticoccidial, anticonvulsant, anti-inflammatory, antidepressant, antimalarial, antioxidant, antileukemic, and antileishmanial activities and other activities. Being considered as advantaged scaffold, the alteration is made with different substituent.
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Pan, Wan-Chen, Mei-Mei Zhang, Jian-Quan Liu, and Xiang-Shan Wang. "Silver Triflate Catalyzed Synthesis of Isoquinolino[2,1-a]quinazo­lino[3,2-c]quinazoline Derivatives via Alkyne Hydroamination." Synthesis 51, no. 16 (2019): 3101–8. http://dx.doi.org/10.1055/s-0037-1611808.

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Using 2-(2-aminophenyl)quinazolin-4(3H)-one and 2-(2-phenylethynyl)benzaldehyde as the reactants, silver triflate (AgOTf) was proved to be an efficient catalyst to promote not only quinazoline cyclization, but also the intramolecular hydroamination of alkyne for the synthesis of 6-aryl-17H,18aH-isoquinolino[2,1-a]quinazolino[3,2-c]quinazolin-17-one derivatives in high yields.
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Alla, Manjula, Gal Potuganti, and Divakar Indukuri. "An Efficient One-Pot Multicomponent Synthesis of Tetracyclic Quinazolino[4,3-b]quinazolines by Sequential C–N Bond Formation and Copper-Mediated Aerobic Oxidative Cyclization." Synlett 29, no. 13 (2018): 1717–22. http://dx.doi.org/10.1055/s-0036-1591578.

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An efficient one-pot synthesis of quinazolino[4,3-b]quinazoline derivatives has been accomplished, starting from 2-(2-bromo­phenyl)quinazolin-4(3H)-one, aldehydes, and various nitrogen sources under aerobic conditions. The multicomponent protocol is mediated by copper(I) salts and involves amination of 2-(2-bromophenyl)quinazolin-4(3H)-one, followed by condensation with the aldehyde and an oxidative cyclization to give the target compounds in moderate to good yields.
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Peter Osarodion Osarumwense, Mary Olire Edema, and Cyril Odianosen Usifoh. "Synthesis and antibacterial activities of quinazolin-4(3h)-one, 2-methyl-4(3h)-quinazolinone and 2–phenyl-4(3h)-quinazolinone." International Journal of Biological and Pharmaceutical Sciences Archive 1, no. 2 (2021): 077–84. http://dx.doi.org/10.30574/ijbpsa.2021.1.2.0027.

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Background: Quinazoline and quinazolinone scaffolds represent an important class of biologically active nitrogen heterocyclic compounds. Many marketed drugs are based on these moieties. A diverse range of molecules with quinazoline/quinazolinone moieties have been reported to exhibit broad spectrum of biological activities Objective: This study is aimed at the synthesis of these quinazolinone derivatives, quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one and evaluate them for their antibacterial activities. Method: The consolidation of 2-amino-methyl-4-methoxybenzoate with acetic anhydride produced the cyclic compound 2-methyl-4, 5-disubstituted-1, 3-benzo-oxazine-4-one which also produce a novel 2,3-disubstituted quinazolin-4 ones via the reaction with hydrazine hydrate. The quinazolinone derivatives quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one were evaluated pharmacologically for their in vivo analgesic activities by acetic acid induced writhing in mice. The compounds synthesized were assuredly validated by means of Infrared, Nuclear Magnetic Resonance (1H and 13C), Gas Chromatography Mass Spectrophotometer and Elemental analysis. The synthesized compounds were tested for their antibacterial activity.Compounds 1,2 and 3 showed significant antibacterial activities. Discussion: Compound 1 was identified by the absence of methyl group and the presence of methyl group for compound 2. The test analysed compounds exhibited significant antibacterial activities. The compounds synthesized exhibited promising antibacterial activities against the tested organisms. Conclusion: The compounds have high antibacterial activities. Compound 2 has a higher activity compared to Compound 1 and 3. Compound 2 has a higher antibacterial against Escherichia coli, Klebsiella pneumonia and Pseudomonas aeuriginosa
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Widiyana, Anita Puspa. "COMPUTATION DESIGN OF QUINAZOLINE-4(3H)-ON DERIVATIVES AS CYCLOOXYGENASE-2 (COX-2) INHIBITOR." Jurnal Farmasi Sains dan Praktis 7, no. 2 (2021): 163–70. http://dx.doi.org/10.31603/pharmacy.v7i2.4827.

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 The 3-(benzylideneamino)-2-(2,4-dichlorophenyl)-quinazoline-4(3H)-ones (BDCQ) are compounds developed as anticancer drugs and quinazolines. The activity and bioavailability of BDCQ derivatives as anticancer compounds that inhibit COX-2 can be predicted by computer programs and online servers. Substituents are added at positions 2 and 3 to the quinazoline-4(3H)-on ring, such as -H, -NO2, -OCH3, -N(CH3)2, -SO2NH2, -OH, and –OCH3. QSAR as COX-2 inhibitor analysis was performed by SPSS Ver. 21 software. Lipinski’s rule of five for determining bioavailability is performed by an online server at http://ilab.acdlabs.com. The best QSAR equation used to predict the COX-2 inhibitors from these compounds is RS-pred = 0.372 Log P + 0.014 MR + 0.979 Etot – 4.859, with n= 12, R = 0.998; SE = 0.356, F = 805.252 and sig = 0.001. Six compounds were predicted to have good oral bioavailability, such as 3-(benzylideneamino)-2-(2,4-dichlorophenyl)quinazoline-4(3H)-one, 2-(2,4-dichlorophenyl)-3-((2-nitrobenzylidene)amino)quinazoline-4(3H)-one, 2-(2,4-dichlorophenyl)-3-((3-nitrobenzylidene)amino)quinazoline-4(3H)-one, 2-(2,4-dichlorophenyl)-3-((2-methoxybenzilidene)amino)quinazoline-4(3H)-one, 2-(2,4-dichlorophenyl)-3-((3-methoxybenzylidene)amino)quinazolin-4(3H)-one, and 2-(((2-(2,4-dichlorophenyl)-4-oxoquinazolin-3(4H)-yl)imino)methyl)- benzenesulfonamide. This research can be used as an in vitro and in vivo study for BDCQ derivatives as anticancer drugs.
 
 
 
 
 
 
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Aly, A. A. "Synthesis And Antimicrobial Activity Of Some Annelated Quinazoline Derivatives." Zeitschrift für Naturforschung B 61, no. 8 (2006): 1012–20. http://dx.doi.org/10.1515/znb-2006-0814.

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A highly efficient and versatile synthetic approach to the synthesis of annelated quinazoline derivatives viz. 3,4,9,10a-tetraazaphenanthrenes 5 - 7, thiazolidinylquinazoline 9, 2,4,9,10a-tetraazaphenanthrene 11, quinazolino[4,3-b]quinazolin-8-one 12 and imidazoquinazolines 14a,b, 15. Also, a variety of pyrazolylquinazolines 19 - 21, pyrimidinylquinazolines 22a,b were obtained via a sequence of heterocyclization reactions of 4-methyl-N-[4-(4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]benzenesulfonamide (2) with different reagents. The new compounds were synthesized with the objective of study their antimicrobial activity
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Martynenko, Yulya, Oleksii Antypenko, Inna Nosulenko, Galina Berest, and Sergii Kovalenko. "Directed Search of Anti-inflammatory Agents Among (3HQuinazoline- 4-ylidene)hydrazides of N-protected Amino acids and their Heterocyclization Products." Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry 19, no. 1 (2020): 61–73. http://dx.doi.org/10.2174/1871523018666190115092215.

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Background: (Quinazoline-4-ylidene)hydrazides are valued intermediates in modern organic chemistry, as they are commonly used for the synthesis of substituted [1,2,4]triazolo[1,5-c]quinazolines. Objective: Unknown N-acyl-2-([1,2,4]triazolo[1,5-c]quinazoline-2-yl)-alkyl-(alkaryl-, aryl-) amines were synthesized and evaluated for anti-inflammatory potential. Methods: The peculiarities of the synthesized compounds structures were studied by IR-, NMR spectroscopy and chromatography-mass spectrometry and were discussed in detail. Probable molecular mechanisms of activity (inhibition of COX-1 and COX-2) were predicted due to molecular docking. Anti-inflammatory activity of synthesized compounds was determined by their ability to reduce the formalin-induced paw edema in rats. Diclofenac sodium was used as reference drug. Results: In this study, the synthesis of N-acetyl-(benzoyl)-2-([1,2,4]triazolo[1,5-c]quinazolinе- 2-yl)alkyl-(aralkyl-, aryl-)amines, using (3H-quinazoline-4-ylidene)hydrazides of Nprotected amino acids or 4-hydrazinoquinazoline and N-prorotected amino acids as starting compounds was developed. It was established that the reaction of (3H-quinazoline-4- ylidene)hydrazides of Boc-amino acids occurred with the formation of N-acetyl-substituted triazoloquinazolines. High anti-inflammatory activity was detected for unknown (3Hquinazoline- 4-ylidene)hydrazides Boc-amino acids (1.13-1.15) and N-acetyl-(benzoyl)-2- ([1,2,4]triazolo[1,5-c]quinazoline-2-yl-)aralkyl-(aryl-)amines (3.2, 3.3, 3.11, 3.12), using the experimental formalin test. Conclusion: The conducted SAR-analysis allowed to detect critical fragments. Namely, the Boc-aminoaralkyl-(aryl-)acid residue in (3H-quinazoline-4-ylidene)hydrazides (1.13- 1.15), benzyl and phenyl linker groups in N-acetyl-(benzoyl)-2-([1,2,4]triazolo[1,5- c]quinazoline-2-yl-)aralkyl-(aryl-) amines (3.2, 3.3, 3.11, 3.12) are believed to be substantial for anti-inflammatory activity.
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Alkhathlan, H. Z., M. A. Al-Saad, H. M. Al-Hazimi, K. A. Al-Farhan, and A. A. Mousa. "Quinazoline, Pyrazolo[1,5-c]Quinazoline and Spiro Quinazoline Dimers from the Reaction of 2-Aminoacetophenone Hydrazones with Triphosgene." Journal of Chemical Research 2002, no. 12 (2002): 587–88. http://dx.doi.org/10.3184/030823402103170952.

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The reaction of hydrazones of 2-aminoacetophenone with triphosgene in dichloromethane or benzene in the presence of triethylamine gave quinazolines, pyrazolo[1,5-c]quinazoline and spiro quinazoline dimers. The latter compounds are being reported for the first time. In addition, a 4,4-disubstituted quinazoline derivative is prepared and its x-ray crystal structure is reported.
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Dissertations / Theses on the topic "Quinazoline"

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Xu, Lu. "New quinazoline analogues as NF-κB activation inhibitors". Scholarly Commons, 2013. https://scholarlycommons.pacific.edu/uop_etds/152.

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NF-κB is a transcription factor protein complex that plays an important role in some cancers and inflammatory responses. It can enhance the proliferation rate, reduce apoptosis, as well as create more blood flow to ensure the survival of cancer. Thus blocking the NF-κB pathway has potential therapeutic benefit. We designed a series of compounds based on quinazoline scaffold pharmacophore model which may have high binding affinity with p50 subunit of NF-κB. The compound series with phenyl substitution at position 2 of quinazoline proved to be more effective at inhibiting NF-κB function both theoretically and experimentally. These compounds also reduce the proliferation of numerous tumor cell lines and the mean GI50 for representative compound 2a is 2.88μM on NCI 60 cell lines. Compound 2a can induce significant apoptosis at the concentration of 1μM. The exploration of the mechanism of action of these compounds found that 2a does not inhibit kinases upstream of NF-κB and does not inhibit p65 translocation from the cytosol to the nucleus as 2b does. However 2a inhibits NF-κB dependent Luciferase expression as well as NF-κB target genes better than 2b. This may suggest that 2a inhibits the NF-κB pathway by directly blocking gene transcription, while 2b acts at cytoplasmic stage.
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El, Ghammarti Samira. "Étude des voies de synthèse de bioisostères de la néothramycine." Lille 1, 1995. http://www.theses.fr/1995LIL10182.

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La néothramycine est une entité connue pour ses propriétés antitumorales ; elle appartient à la famille des pyrrolobenzodiazépines dont le chef de file est l'anthramycine. La néothramycine se distingue des autres membres de cette famille par sa faible toxicité. D'un point de vue chimique, la synthèse de ces systèmes cycliques reste assez délicate car ils possèdent la fonction carbinolamine (ou son équivalent chimique) qui est très réactive et un carbone asymétrique dont la configuration (s) est indispensable à l'activité biologique. Nous nous sommes intéressés aux voies de synthèse permettant de remplacer le cycle pyrrolidine de la néothramycine par un cycle pyroglutamique, dont l'atome d'azote en position (4) est basculé à la position (11a). Par modélisation moléculaire, nous avons pu constater qu'une parfaite superposition s'établit entre la néothramycine qui est le modèle naturel et la molécule conçue partant de l'acide L-pyroglutamique. Nous avons notamment étudié la N-alkylation du pyroglutamate de méthyle N-silylé et de l'acide pyroglutamique N,O-disilylé par des amides aromatiques N-chlorométhylés. Ces derniers sont préparés à partir des amides aromatiques correspondants de formol et de chlorotriméthylsilane. Cette méthode est généralisable aux esters pyroglutamiques. La réaction de Friedel-Crafts des acides pyroglutamiques N-substitués, catalysée par différents acides de Lewis (AlCl3, SnCl4, AlBr3) ou par un mélange de CF3COOH/(CF3CO)2O, s'accompagne toujours d'une décarbonylation et les produits isolés sont alors des benzopyrimidines. Dans certaines conditions de catalyse (BF3,CF3SO3H), une décomposition de type retro Mannich est prépondérante. D'autres tentatives de cyclisation ont été réalisées (Grignard, Vilsmeier-Haack, Friedel-Crafts intermoléculaire), catalyse par l'ion F- d'intermédiaire phénolique silylé, utilisation du réactif de Meerwein) ont aussi échouées. Néanmoins, nous avons étudié quelques aspects de la réactivité chimique de ces produits. En outre, ces composés tricycliques seront testés au National Cancer Institute.
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Dade, Jöel. "Synthèse d'hétérocycles azotés quinoléiques et quinazoliniques à visée antileishmanienne." Paris 11, 2004. http://www.theses.fr/2004PA114811.

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Ce travail de thèse consiste en la synthèse d'hétérocycles azotés originaux dérivé de quinoléines et de quinazolines. Ces composés sont des analogues structuraux de quinoléines naturelles de type Chimanine douées d'activité antileishmanienne. Nous avons, au cours de ce travail, préparé une centaine de quinoléines et quinazolines qui ont été évaluées contre Leishmania donovani donovani, et leishmania amazonensis. Des tests en vue d'une recherche d'activité antipaludique sont également en cours. Nous avons également étudié la réactivité des quinazolines substituées par un époxyde en position 2 vis-à-vis de divers agents nucléophiles (organolithiens, réactifs de Grignard, amines)<br>This thesis consists in the synthesis of nitrogen heterocyclic compounds derived from quinolines and quinazolines. These compounds are structurally analogues to natural quinolines, the chimanines, having antileishmanial activity. During this work we have prepared about a hundred quinolinic and quinazolinic compounds and we have evaluated their activity against Leishmania donovani donovani and Leishmania amazonensis strains. Biological evaluation against Plasmodium falciparum is currently carry out. We also studied the reactivity of quinazolines substituted at the 2 position by an epoxy group towards nucleophilic reagents such as organolithium, Grignard reagents and amino compounds
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Zeghida, Walid. "Conception et Synthèse d'Hétérocycles Azotés Polyfonctionnalisés Biologiquement Actifs: Des Acridines aux Quinazolines." Phd thesis, Grenoble 1, 2007. http://www.theses.fr/2007GRE10254.

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Ce travail porte sur la conception de dérivés d’aminoacridine et de quinazoline. Dans une première partie, nous avons préparé des dérivés d’aminoacridine ortho-hydroxyméthylée. Pour synthétiser ces dérivés nous avons mis au point une stratégie efficace et générale mettant en jeu la préparation d’un intermédiaire-clé qui peut ensuite être fonctionnalisé. A partir de ce dernier nous avons préparé des dérivés substitués par un motif guanidine. Nous avons également préparé un dérivé iodé afin d’étudier sa distribution cellulaire par microscopie ionique (SIMS). Les propriétés biologiques (IC50 et distribution cellulaire) de ces nouveaux composés ont été évaluées sur des cellules cancéreuses et les résultats obtenus ont confirmé l’intérêt de cette nouvelle famille d’aminoacridine comme anticancéreux. Dans une seconde partie nous avons mis au point une nouvelle méthodologie de synthèse de 2-alkylamino-4(3H)-quinazolinones. Nous avons ainsi préparé différents dérivés comportant un motif quinazolinone à partir d’amines aromatiques et hétérocycliques. Certains de ces dérivés ont fait l’objet d’études biologiques préliminaires (effet cytostatique, ligand ADN-quadruplex) et les résultats obtenus sont très encourageants<br>This work concerns the design of aminoacridine and quinazoline derivatives. In a first part, we have prepared ortho-hydroxymethyl aminoacridine derivatives. To synthesize these derivatives we designed an effective and general strategy involving the preparation of a key- intermediate that can be functionnalised. We therefore prepared derivatives substituted by a guanidine moiety. We also prepared a derivative substituted with an iodine atom to study its cellular distribution by ionic microscopy (SIMS). The biological properties (IC50 and cellular distribution) of these new compounds have been investigated on various cancer cells and the data point out the interest of this new family of aminoacridine as anticancer dyes. In a second part we designed a new methodology of synthesis of 2-alkylamino-4(3H)-quinazolinones. We have prepared various derivatives containing a quinazolinone moiety from aromatic and heterocyclic amines. Some of these derivatives were given for preliminary biological studies (IC50, DNA-quadruplex ligand) and the first results are very encouraging
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Zeghida, Walid. "Conception et Synthèse d'Hétérocycles Azotés Polyfonctionnalisés Biologiquement Actifs: Des Acridines aux Quinazolines." Phd thesis, Université Joseph Fourier (Grenoble), 2007. http://tel.archives-ouvertes.fr/tel-00221136.

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Ce travail porte sur la conception de dérivés d'aminoacridine et de quinazoline. Dans une première partie, nous avons préparé des dérivés d'aminoacridine ortho-hydroxyméthylée. Pour synthétiser ces dérivés nous avons mis au point une stratégie efficace et générale mettant en jeu la préparation d'un intermédiaire-clé qui peut ensuite être fonctionnalisé. A partir de ce dernier nous avons préparé des dérivés substitués par un motif guanidine. Nous avons également préparé un dérivé iodé afin d'étudier sa distribution cellulaire par microscopie ionique (SIMS). Les propriétés biologiques (IC50 et distribution cellulaire) de ces nouveaux composés ont été évaluées sur des cellules cancéreuses et les résultats obtenus ont confirmé l'intérêt de cette nouvelle famille d'aminoacridine comme anticancéreux.<br />Dans une seconde partie nous avons mis au point une nouvelle méthodologie de synthèse de 2-alkylamino-4(3H)-quinazolinones. Nous avons ainsi préparé différents dérivés comportant un motif quinazolinone à partir d'amines aromatiques et hétérocycliques. Certains de ces dérivés ont fait l'objet d'études biologiques préliminaires (effet cytostatique, ligand ADN-quadruplex) et les résultats obtenus sont très encourageants.
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Larraufie, Marie-Hélène. "Development of new radical cascades and multi-component reactions : application to the synthesis of nitrogen-containing heterocycles." Paris 6, 2011. http://www.theses.fr/2011PA066516.

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Le travail décrit dans ce manuscrit de thèse est consacré au développement de nouvelles méthodes radicalaires et organométalliques permettant la synthèse de différentes classes de polycycles azotés. Nous avons étudié des cascades impliquant le motif N-acylcyanamide. Des précurseurs de type alkyle ont permis la synthèse de quinazolinones naturelles. L’utilisation de précurseurs vinyliques a permis de mettre à jour un processus de migration original, qui apporte de nouveaux éléments pour la compréhension du mécanisme de substitution aromatique homolytique. Enfin des radicaux aminyles ont pu être engagés dans ces cascades, conduisant à la première synthèse radicalaire de guanidines. Conscients de la nécessité de trouver des alternatives vertes pour la génération de radicaux, nous nous sommes intéressés à la catalyse photoredox en lumière visible. Nous l’avons utilisée pour la photo-génération de radicaux à partir d’époxydes et d’aziridines. D’autre part, le système catalytique palladium/norbornene a été employé pour la synthèse efficace de phenanthridines à partir d’iodures d’aryles et d’amines benzyliques. L’utilisation d’amide benzyliques nous a permis de mettre à jour la première exception à l’effet ortho. Des calculs DFT ont rationnalisé l’influence de la chélation sur la sélectivité de l’élimination réductrice à partir de l’intermédiaire Pd(IV) impliqué
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Li, Jiyang [Verfasser]. "Investigation of Phthalazine, Quinazoline and Pyrimidine Derivatives as ABCG2 Inhibitors / Jiyang Li." Bonn : Universitäts- und Landesbibliothek Bonn, 2018. http://d-nb.info/1167857135/34.

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Malecki, Natacha. "Conception et synthese de derives quinoleiniques et quinazoliniques inhibiteurs potentiels des topoisomerases i et ii." Lille 2, 2001. http://www.theses.fr/2001LIL2P251.

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Chibani, Aïssa. "Électrosynthèse d'hétérocycles azotes du type quinoléine, quinazoline et triazine par réduction de nitrobenzènes o-substitues." Rennes 1, 1992. http://www.theses.fr/1992REN1A004.

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Marks, Kevin Randall. "Investigating the fluoroquinolone-topoisomerase interaction by use of novel fluoroquinolone and quinazoline analogs." Diss., University of Iowa, 2011. https://ir.uiowa.edu/etd/1018.

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Fluoroquinolones are broad-spectrum antibacterial agents based on the structure of nalidixic acid. For nearly five decades it has been known that fluoroquinolones inhibit bacterial growth by blocking the enzymatic action of type II topoisomerases such as DNA gyrase and topoisomerase IV. Only recently has it been discovered that some fluoroquinolones are capable of a mechanism that results in fragmented DNA and leads to rapid bacterial cell death. This mechanism is not well understood. Presented here are studies towards understanding the structure activity relationship (SAR) of fluoroquinolones, specifically to determine what leads to the novel mechanism termed "rapid lethality." This work is based on the hypothesis that structurally unique fluoroquinolones interact with the DNA-topoisomerase complex in a unique manner that ultimately leads to rapid cell death. The first approach to understand SAR for killing was to evaluate the effect of a ring fusion between N-1 and C-8 of the fluoroquinolone core. Known lethal fluoroquinolones are substituted by N-1 cyclopropyl and C-8 methoxy, but some clinically important fluoroquinolones contain a 2-methylmopholino moiety between these two positions. Novel fluoroquinolones were synthesized and clinically available agents were obtained to create a panel of drug molecules with one of six C-7 substituents and either the morpholine ring system or N-1 cyclopropyl and C-8 methoxy. Bacteriostatic and bactericidal activities of these compounds were determined. Bactericidal studies were conducted both in the presence and absence of chloramphenicol, a protein synthesis inhibitor used to simulate non-growing bacteria. Lethality in the presence of chloramphenicol is also important when considering co-administration of fluoroquinolones with other antibiotic classes. In a second study, fluoroquinolones were synthesized with a C-2 thioalkyl substitution. Substitutions at the C-2 position are severely lacking in clinical fluoroquinolones, with only prulifloxacin, a newly developed antibiotic, being substituted by an N-1 to C-2 thiazetidine ring structure. Analogs of ciprofloxacin and moxifloxacin were synthesized such that the N-1, C-2, and C-8 positions were substituted with cyclopropyl, thioethyl/thioisopropyl, and methoxy groups, respectively. The compounds were then evaluated for antibiotic activity against three different bacterial strains to evaluate the contribution of the C-2 thioalkyl substituent to antibacterial activity. In a third study, quinazoline-2,4-diones, a new antibiotic class structurally and mechanistically similar to fluoroquinolones, were modified at the C-4 position in an effort to understand the binding interaction between these compounds and the target enzyme. Importantly, the quinazoline-2,4-diones typically retain activity against bacterial cells known to be resistant to fluoroquinolones and are less likely to select for resistant mutants. In this study, the C-4 carbonyl was replaced with either a thiocarbonyl or a hydroxylimine and the new compounds, bearing C-7 substituents common to potent antibiotic fluoroquinolones and quinazolines, were evaluated for activity against bacterial cells. Despite the findings of recently published X-ray crystallography, it was determined that one of the greatest determinants in antibiotic activity of fluoroquinolones is the C-7 substituent. Additionally, there is increasing evidence that the C-2 carbonyl of quinazoline-2,4-diones affords the increase in activity against resistant mutants by creating a unique binding interaction. Collectively, the conclusions reached here add to our understanding of the structure activity relationship of the fluoroquinolone antibiotic class for rapidly killing bacterial cells and overcoming resistant mutants.
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Books on the topic "Quinazoline"

1

Brown, D. J. Quinazolines. Wiley, 1996.

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Feldmann, Burkhard. Darstellung und spektroskopische Eigenschaften neuer H-Chelate der Chinazolinreihe. Hartung-Gorre, 1986.

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Gamal Al-kaf, Ali, ed. Quinazolinone and Quinazoline Derivatives. IntechOpen, 2020. http://dx.doi.org/10.5772/intechopen.85315.

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Quinoxalines. Wiley, 2004.

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Brown, Desmond J. Quinazolines, Supplement 1. Wiley & Sons, Incorporated, John, 2007.

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Brown, Desmond J. Quinazolines, Supplement 1. Wiley & Sons, Incorporated, John, 2009.

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Joshi, B. L. Some studies with quinazolines and related compounds. 1985.

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Qualmann, Christiane. Multidrug-resistente menschliche lymphoblastoide T-Zellinien als Modell zur Charakterisierung des Kreuzresistenzverhaltens neuer Zytostatika: Untersuchung von Quinazolin- und Anthrapyrazol-Derivaten. 1992.

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Book chapters on the topic "Quinazoline"

1

Barker, A. J., L. R. Hughes, P. Warner, K. Burrows, and A. L. Jackman. "Thymidylate Synthase Inhibition of Modified Quinazoline Antifolates." In Cytotoxic Anticancer Drugs: Models and Concepts for Drug Discovery and Development. Springer US, 1992. http://dx.doi.org/10.1007/978-1-4615-3492-1_4.

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Gros, Philippe C. "Other Stoichiometric Metalation Reactions on Pyrimidine and Quinazoline." In Topics in Heterocyclic Chemistry. Springer Berlin Heidelberg, 2012. http://dx.doi.org/10.1007/7081_2012_93.

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Kolarovič, Andrej. "Lithiations and Grignard Reactions on Pyrimidine and Quinazoline." In Topics in Heterocyclic Chemistry. Springer Berlin Heidelberg, 2012. http://dx.doi.org/10.1007/7081_2012_94.

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Panwar, Vivek, Kritika Mukherji, Manjunath Ghate, Deepak K. Jindal, and Deepak Kumar. "EGFR-Targeted Quinazoline Clubbed Heterocycles as Anticancer Agents." In Biomedical Translational Research. Springer Nature Singapore, 2022. http://dx.doi.org/10.1007/978-981-16-9232-1_21.

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Dangi, R. R., N. S. Chundawat, and K. L. Ameta. "Synthesis and Biological Evaluation of Some Quinazoline Heterocyclic Derivatives." In Green Chemistry: Synthesis of Bioactive Heterocycles. Springer India, 2014. http://dx.doi.org/10.1007/978-81-322-1850-0_13.

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da Silva, Maria Fátima das Graças Fernandes, João Batista Fernandes, Moacir Rossi Forim, Paulo Cezar Vieira, and Israel Cívico Gil de Sá. "Alkaloids Derived from Anthranilic Acid: Quinoline, Acridone, and Quinazoline." In Natural Products. Springer Berlin Heidelberg, 2013. http://dx.doi.org/10.1007/978-3-642-22144-6_25.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of nickel(II) complex with quinazoline ligand." In Magnetic Properties of Paramagnetic Compounds, Magnetic Susceptibility Data, Volume 5. Springer Berlin Heidelberg, 2022. http://dx.doi.org/10.1007/978-3-662-65098-1_321.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of manganese(II) complex with quinazoline ligand." In Magnetic Properties of Paramagnetic Compounds, Magnetic Susceptibility Data, Volume 5. Springer Berlin Heidelberg, 2022. http://dx.doi.org/10.1007/978-3-662-65098-1_56.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of cobalt(II) complex with quinazoline ligand." In Magnetic Properties of Paramagnetic Compounds, Magnetic Susceptibility Data, Volume 5. Springer Berlin Heidelberg, 2022. http://dx.doi.org/10.1007/978-3-662-65098-1_245.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of copper(II) complex with quinazoline ligand." In Magnetic Properties of Paramagnetic Compounds, Magnetic Susceptibility Data, Volume 5. Springer Berlin Heidelberg, 2022. http://dx.doi.org/10.1007/978-3-662-65098-1_411.

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Conference papers on the topic "Quinazoline"

1

Guerreiro Souzedo, Gabriela, LJUBICA TASIC, and Caio Henrique Nasi De Barros. "Synthesis of Quinazoline Derivatives for Adenosine Kinase Inhibition." In XXV Congresso de Iniciação Cientifica da Unicamp. Galoa, 2017. http://dx.doi.org/10.19146/pibic-2017-78452.

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Fadil MOUSA, Enaam, and Ibtissam Khalifa JASSIM. "SYNTHESIS ,CHARACTERIZATION AND BIOLOGICAL ACTIVITY STUDY OF SOME HETEROCYCLIC COMPOUNDS." In IV.International Scientific Congress of Pure,Appliedand Technological Sciences. Rimar Academy, 2022. http://dx.doi.org/10.47832/minarcongress4-18.

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Heterocycles are an important class of organic compounds because of their applications in medicines and industrial fields. Therefore our study included preparation of these compound such as oxazepine and quinazoline rings, which were prepared through two steps: The first step included the reaction of the Schiff bases derived from sulfamethaxazole (1-4) with each of phthalic anhydride and 3- nitrophthalic anhydride for the preparation of oxazepines (5-12) .While the second step included the preparation of quinazoline compounds (13-16) from the reaction of Schiff bases (1-4) with anthranilic acid using dry benzene as a medium and solvent for the reaction. All prepared compounds were characterized by using infrared,proton- nuclear magnetic resonance, mass techniques and melting points, and their purity was determined by thin layer chromatography technique also screened the biological activity of some of these prepared compounds by using two types of bacteria Gram-positive and negative . The results showed that these compounds have a good inhibition against these organisms
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Militaru, Andra, Adriana Smarandache, Abdallah Mahamoud, et al. "Stability Characterization of Quinazoline Derivative BG1188 by Optical Methods." In ADVANCES IN LASEROLOGY - SELECTED PAPERS OF LASER FLORENCE 2010: The 50th Birthday of Laser Medicine World. AIP, 2011. http://dx.doi.org/10.1063/1.3626907.

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Kumar, Balbir, Naresh Sharma, Asif Ali, and Vivek K. Gupta. "Crystallographic structure analysis of 4-phenoxy-2-(4-(trifluoromethyl)phenyl) quinazoline." In NATIONAL CONFERENCE ON RECENT ADVANCES IN EXPERIMENTAL AND THEORETICAL PHYSICS (RAETP-2018). Author(s), 2018. http://dx.doi.org/10.1063/1.5051271.

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Fatykhov, Ramil F., Igor A. Khalymbadzha, Vladimir L. Rusinov, and Oleg N. Chupakhin. "Modification of 1-hydroxy-3-methoxy-10-methylacridone by quinazoline and quinoxalone." In PROCEEDINGS OF INTERNATIONAL CONFERENCE ON RECENT TRENDS IN MECHANICAL AND MATERIALS ENGINEERING: ICRTMME 2019. AIP Publishing, 2020. http://dx.doi.org/10.1063/5.0028211.

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Tojiboev, Akmaljon, Sherzod Zhurakulov, Ulli Englert, et al. "Hirshfeld surface analysis and energy framework for crystals of quinazoline methylidene bridged compounds." In The 2nd International Online Conference on Crystals. MDPI, 2020. http://dx.doi.org/10.3390/iocc_2020-07235.

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OuYang, Yiqiang, Chen Chen, Ping Wang, Chao Sun, WuFu Zhu, and Shan Xu. "Synthesis of N-4-(4-chloro-3-trifluoromethyl-phenyl)-7-methoxy-quinazoline-4,6-diamine." In 2015 2nd International Conference on Machinery, Materials Engineering, Chemical Engineering and Biotechnology. Atlantis Press, 2016. http://dx.doi.org/10.2991/mmeceb-15.2016.158.

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Christopher, Williams, Larroque Anne‐Laure, Huang Ying, et al. "Abstract A142: Molecular modeling approach to the rational design of promiscuous quinazoline‐based EGFR inhibitors." In Abstracts: AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics--Nov 15-19, 2009; Boston, MA. American Association for Cancer Research, 2009. http://dx.doi.org/10.1158/1535-7163.targ-09-a142.

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Yen, Shih Chieh, Shao-Zheng Peng, Hung-Jyun Huang, et al. "Abstract 2809: Novel 2,5,8-trihydro-6,7-disubstituted-4-(3'-alkylsulfonamidoanilino) quinazoline derivatives as RAF inhibitor." In Proceedings: AACR Annual Meeting 2018; April 14-18, 2018; Chicago, IL. American Association for Cancer Research, 2018. http://dx.doi.org/10.1158/1538-7445.am2018-2809.

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Ayvazyan, A. S., A. I. Markosyan, F. H. Arsenyan, and Kh S. Hakobyan. "SYNTHESIS AND BIOLOGICAL ACTIVITY OF SPIRO[BENZO[H]QUINAZOLINE-5,1’-CYCLOHEPTANE]- 4(6H)-ONE DERIVATIVES." In MedChem-Russia 2021. 5-я Российская конференция по медицинской химии с международным участием «МедХим-Россия 2021». Издательство Волгоградского государственного медицинского университета, 2021. http://dx.doi.org/10.19163/medchemrussia2021-2021-240.

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