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Journal articles on the topic 'Quinazolinon'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

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. Quin

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2

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-o

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3

R., S. VARMA, and PREETI GUPTA (Miss). "Nucleophilic Reactions of 2-Methyl-3-( 4' -carbomethoxyphenyl)-4-quinazolinones with 2-lndolinones." Journal of Indian Chemical Society Vol. 66, Nov 1989 (1989): 804–5. https://doi.org/10.5281/zenodo.6090915.

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Department of Chemistry, Lucknow University, Lucknow-226 007 <em>Manuscript received 10 March 1989, accepted 20 June 1989</em> 2-Methyl-3-(4'-carbomethoxphenyl)-4-quinazolinone undergoes nucleophilic addition-elimination reactions with different lndolinones leading to 2-(3-methylene- substituted-oxindolyl)-3-(4'-carbomethoxyphenyl)-4-quinazolinones (2a- e), Similarly, <em>N</em>-methylindolinones react with 2-methyl-3-(4'-carbomethoxyphenyl)-4-quinazolinone to give 2- (3-methylene-1- methyl-substituted -oxindolyl)- 3 -( 4' - carbomethoxyphenyl)-4 quinazolinones (4a -e). Mannich

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4

S, G. ABDEL-HAMIDE. "Synthesis of some New Heterocyclic Systems bearing 2-Phenyl-6-iodo-4(3H)-quinazolinon-3-yl Moiety as Antibacterial Agents." Journal of Indian Chemical Society Vol. 74, Aug 1997 (1997): 613–18. https://doi.org/10.5281/zenodo.5891302.

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Pharmaceutical Chemistry Department, Al-Azhar University, Cairo, Nasr City, Egypt <em>Manuscript received 6 March 1995, revised 18 March 1996, accepted 24 July 1996</em> A number of heterobicyclic systems bearing 2-phenyl-6-iodo-4(3<em>H</em>)-quinazolinon-3-yl moiety have been synthesised by interaction of 3- amino-2-phenyl-6-iodo-4(3<em>H</em>)-quinazolinone with bifunctional compounds followed by cyclisation in different media. Some of the compounds possess high activity aganist bacteria.

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5

Deng, Zhijiang, Jieming Li, Pengbo Zhu, et al. "Quinazolinones as Potential Anticancer Agents: Synthesis and Action Mechanisms." Biomolecules 15, no. 2 (2025): 210. https://doi.org/10.3390/biom15020210.

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Quinazolinones, essential quinazoline derivatives, exhibit diverse biological activities with applications in pharmaceuticals and insecticides. Some derivatives have already been developed as commercial drugs. Given the rising cancer incidence, there is a critical need for new anticancer agents, and quinazolinones show promising potential in this domain. The present review focuses on novel advances in the synthesis of these important scaffolds and other medicinal aspects involving drug design, the structure–activity relationship, and action mechanisms of quinazoline and quinazolinone derivativ

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6

Starikova, Alla Andreevna, Alexandra Aleksandrovna Tsibizova, and Marina Aleksandrovna Samotrueva. "BIOLOGICAL ACTIVITY OF NATURAL QUINAZOLINE ALKALOIDS." Chemistry of plant raw material, no. 2 (May 4, 2025): 47–73. https://doi.org/10.14258/jcprm.20250214908.

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To date, quinazoline alkaloids of natural origin, as well as synthetic derivatives based on them, whose structure contains an aromatic heterocyclic system including a pyrimidine cycle and a benzoin ring connected to it, are promising according to the criterion of the optimal profile of pharmacological activity. Currently, several hundred compounds of the quinazoline nature have been identified with a wide range of biological activities, including psychotropic (antidepressant, antipsychotic, sedative, hypnotic, anticonvulsant, etc.), antiplatelet, hypotensive, anti-inflammatory, antioxidant and

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7

Khachatryan, D. S., V. A. Misyurin, M. A. Baryshnikova, N. V. Golubtsova, A. V. Kolotaev, and K. R. Matevosyan. "Quinazolinon derivatives for the treatment of neoplastic, parasitic and neurodegenerative diseases." Russian Journal of Biotherapy 16, no. 3 (2017): 32–42. http://dx.doi.org/10.17650/1726-9784-2017-16-3-32-42.

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In this review we discuss some biological activities of quinazolinon derivatives. The derivatives of quinazolinon possess their activity by binding to some proteins important for the survival, proliferation and metastasis of tumor cells. There are grounds to initiate clinical trials of these substances to create new treatment protocols for a wide range of cancer diseases, several parasitic diseases, and certain neurodegenerative diseases.

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8

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-

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9

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 demon

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10

Jianghong, Man, Qi Jianbin, Jiang Jie, and Li Sha. "Microwave Reaction Improved Heterocyclization of Quinazolinone Ring in Synthesis of Erlotinib Analogues." Journal of Pharmaceutical and Biomedical Sciences 10, no. 05 (2020): 99–105. https://doi.org/10.1234/zenodo.3876.

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Background Tinibs were a kind of important epidermal growth factor receptor (EGFR) inhibitors used as potential therapeutic agents in treating non-small cell lung cancer (NSCLC) in clinic. The drug resistance of clinical used tinibs made the development of more active tinib analogues an attractive field in research. Quinazoline ring was regarded as the key fragment in tinibs and quinazolinone was indispensible intermediate in the synthesis of quinazoline. Thus, synthesis of quinazolinone intermediates was a key step which would further limit the overall yield of final product of tinib analogue

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11

Alsibaee, Aishah M., Hanan M. Al-Yousef, and Huda S. Al-Salem. "Quinazolinones, the Winning Horse in Drug Discovery." Molecules 28, no. 3 (2023): 978. http://dx.doi.org/10.3390/molecules28030978.

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Quinazolines are nitrogen-containing heterocycles that consist of a benzene ring fused with a pyrimidine ring. Quinazolinones, oxidized quinazolines, are promising compounds with a wide range of biological activities. In the pharmaceutical field, quinazolinones are the building blocks of more than 150 naturally occurring alkaloids isolated from different plants, microorganisms, and animals. Scientists give a continuous interest in this moiety due to their stability and relatively easy methods for preparation. Their lipophilicity is another reason for this interest as it helps quinazolinones in

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12

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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13

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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14

Singh, A. "SYNTHESIS OF NOVEL QUINAZOLIN-4(3H)-ONYL AZETIDINONES AS POTENTIAL ANTICONVULSANT AGENTS." INDIAN DRUGS 54, no. 11 (2017): 22–27. http://dx.doi.org/10.53879/id.54.11.10766.

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A series of 4-(substituted aryl)- 1- [2’- methyl-6’- substituted anilino quinazolinon-4’-(3’H)-onyl ] -3- chloroazetidin- 2-ones 14-25 have been synthesized by addition of substituted anilines to 4-(substituted aryl)- 1- [2’- methyl-6’- bromoquinazolinon-4’-(3’H)-onyl ] -3- chloro- azetidin-2-ones 8-13 which in turn were prepared by the cycloaddition of triethylamine in dioxane to 3-(N-substituted benzylidene amino phenyl amido )-2-methyl-6-bromoquinazolin-4(3H)-ones 2-7 in presence of acetyl chloride. These compounds were screened for anticonvulsant activity and acute toxicity. Compound 4-(su

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15

Jianghong, Man, Qi Jianbin, Jiang Jie, and Li Sha. "Microwave Reaction Improved Heterocyclization of Quinazolinone Ring in the Synthesis of Erlotinib Analogues." Journal of Pharmaceutical and Biomedical Sciences 10, no. 05 (2020): 99–105. https://doi.org/10.5281/zenodo.3903346.

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Core tip: Drug resistance caused by point mutations in epidermal growth factor receptor (EGFR) weakened therapeutic efficacy of EGFR inhibitors of tinibs. Thus, the discovery of new tinib analogues of greater efficacy was an attractive focus. As an important intermediate of nitrogen-containing heterocyclic compounds with diverse chemical reactivity and a wide range of biological activity, quinazoline was regarded as an important fragment of tinib analogues. Thus, the synthesis of quinazolinone intermediates was a key step which would limit the overall yield of tinib analogues. Based on this si

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16

Koketsu, Mamoru, Amol Sonawane, Yunnus Shaikh, and Dinesh Garud. "Synthesis of Isoquinoline-Fused Quinazolinones through Ag(I)-Catalyzed Cascade Annulation of 2-Aminobenzamides and 2-Alkynylbenzaldehydes." Synthesis 51, no. 02 (2018): 500–507. http://dx.doi.org/10.1055/s-0037-1610910.

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A new route for the expedient synthesis of a specific regioisomer of isoquinoline-fused quinazolinones is reported. Silver(I)-catalyzed cascade cyclization of 2-aminobenzamides and 2-alkynylbenzaldehydes followed by in situ oxidation gives 12-butyl- or 12-aryl-6H-isoquinolino[2,1-a]quinazolin-6-ones in 69–91% yields. The structure of the isoquinoline-fused quinazolinone was confirmed by X-ray crystallography analysis.

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17

Bhavesh, Amrute B., Amrutkar D. Rakesh, and Tambe R. Santosh. "Design and Molecular Docking Studies of Some 2,3 Di-Substituted Quinazolin-4-One Analogues Against Staphylococcus aureus UDG." Current Computer-Aided Drug Design 16, no. 4 (2020): 402–6. http://dx.doi.org/10.2174/1573409915666190916100437.

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Background: In this present investigation, some 2, 3 disubstituted-quinazolin-4-one derivatives are designed and docked against chain A and chain B of (3WDF) receptor. Methods: The heterocyclic fused rings quinazolinone have drawn a great attention owing to their expanded applications in the field of pharmaceutical chemistry. The diverse range of molecules with quinazoline/quinazolinone moieties have been reported to exhibit a broad spectrum of biological activities. Results: The results designate that the quinazolinone ring forms hydrophobic and hydrogen bond contacts with ASN 127 A, ALA 126

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18

Kut, D., M. M. Kut, M. Yu Onysko, V. V. Pantyo, E. M. Danko, and G. M. Koval. "ANTIMICROBIAL ACTIVITY OF LINEAR CHALCOGEN-FUNCTIONALIZED DERIVATIVES OF THIAZOLO[2,3-b]QUINAZOLINIUM." Scientific Bulletin of the Uzhhorod University. Series «Chemistry» 52, no. 2 (2024): 59–66. https://doi.org/10.24144/2414-0260.2024.2.59-66.

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The study examines the antimicrobial activity of linear chalcogen-functionalized derivatives in the thiazoloquinazoline series against the pathogen Staphylococcus aureus and investigates the influence of low-intensity laser radiation on the sensitivity of thiazolo[2,3-b]quinazoline chlorides. The research involved synthesizing the investigated thiazolo[2,3-b]quinazoline chlorides via chalcogen-induced cyclization. For the first time, 2,3-dihydro-2-((trichloro-λ4-selanyl)methyl)-5-oxo-8-(trifluoromethyl)-5H-thiazolo[2,3-b]quinazolin-10-ium chloride was obtained, and its structure was confirmed

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19

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

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20

Mravljak, Janez, Lara Slavec, Martina Hrast, and Matej Sova. "Synthesis and Evaluation of Antioxidant Properties of 2-Substituted Quinazolin-4(3H)-ones." Molecules 26, no. 21 (2021): 6585. http://dx.doi.org/10.3390/molecules26216585.

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Quinazolinones represent an important scaffold in medicinal chemistry with diverse biological activities. Here, two series of 2-substituted quinazolin-4(3H)-ones were synthesized and evaluated for their antioxidant properties using three different methods, namely DPPH, ABTS and TEACCUPRAC, to obtain key information about the structure–antioxidant activity relationships of a diverse set of substituents at position 2 of the main quinazolinone scaffold. Regarding the antioxidant activity, ABTS and TEACCUPRAC assays were more sensitive and gave more reliable results than the DPPH assay. To obtain

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21

Kulya, D., D. Kut, M. Kut, and M. Onysko. "SYNTHESIS OF 2,3-DIALKENYL DERIVATIVES OF QUINAZOLIN-4-ONE." Scientific Bulletin of the Uzhhorod University. Series «Chemistry» 53, no. 1 (2025): 40–44. https://doi.org/10.24144/2414-0260.2025.1.40-44.

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In the course of this study, alkylation of two starting thiols — 3-allyl-2-mercaptoquinazolin-4-one and 3-methallyl-2-mercaptoquinazolin-4-one — was carried out using allyl bromide and metallyl chloride in an alcoholic-alkaline medium. As a result of these reactions, new 2,3-dialkenyl derivatives of quinazolin-4-one were obtained, which have not been previously reported in the literature. The structures of the newly synthesized compounds were confirmed by NMR spectroscopy (¹H and ¹³C), as well as elemental analysis. The absence of thioamide proton signals in the ¹H NMR spectra indicates that a

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22

Barat, Gaman G., and Mahesh R. Solanki. "Antimicrobial Study of Novel Triazoles Synthesized from Chalcones." Oriental Journal Of Chemistry 40, no. 3 (2024): 794–98. http://dx.doi.org/10.13005/ojc/400322.

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Heterocyclic compound such as quinazoline derivatives shows wide range of medicinal application in the area such as anticonvulsant, antitumor, antifungal, antimalaria, anti-hyperlipidemic and anti-inflammatory etc. activity because of these it shows great interest to study. In the presence study, we have synthesized triazole based quinazolinones by condensation reaction between α-methyl ketone and aromatic aldehydes under ethanol as the solvent to produced chalcones derivatives. This chalcone derivative have α, β-unsaturated part which is enhanced the reactivity of compound. Chalcone further r

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23

Tojiboev, Akmal, Sherzod Zhurakulov, Valentina Vinogradova, Ulli Englert, and Ruimin Wang. "Stereochemistry of the methylidene-bridged quinazoline-isoquinoline alkaloid 3-{[6,7-dimethoxy-1-(4-nitrophenyl)-1,2,3,4-tetrahydroisoquinolin-2-yl]methylidene}-1,2,3,9-tetrahydropyrrolo[2,1-b]quinazolin-9-one methanol monosolvate." Acta Crystallographica Section E Crystallographic Communications 76, no. 6 (2020): 914–19. http://dx.doi.org/10.1107/s2056989020006696.

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Two potentially bioactive fragments, namely a tricyclic quinazoline derivative with an exocyclic alkene moiety and a substituted isoquinoline, are coupled to give 3-{[6,7-dimethoxy-1-(4-nitrophenyl)-1,2,3,4-tetrahydroisoquinolin-2-yl]methylidene}-1,2,3,9-tetrahydropyrrolo[2,1-b]quinazolin-9-one. The target product crystallizes as a methanol solvate, C29H26N4O5·CH4O, and is E configured. The alternative Z isomer would necessarily imply either considerable twist about the central double bond or very unfavourable intramolecular contacts between sterically more demanding substituents. The main res

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24

Tashrifi, Zahra, Mohammad Mohammadi-Khanaposhtani, Mahmood Biglar, Bagher Larijani, and Mohammad Mahdavi. "Isatoic Anhydride: A Fascinating and Basic Molecule for the Synthesis of Substituted Quinazolinones and Benzo di/triazepines." Current Organic Chemistry 23, no. 10 (2019): 1090–130. http://dx.doi.org/10.2174/1385272823666190701142930.

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This review article is focused on the synthesis of compounds with quinazolinones and benzo di/triazepine scaffolds. These invaluable derivatives are of great interest in medicinal and pharmaceutical studies because of their important biological properties. Quinazolinones have diverse applications due to their antibacterial, analgesic, antiinflammatory, antifungal, antimalarial, antihypertensive, CNS depressant, anticonvulsant, antihistaminic, antiparkinsonism, antiviraland and anticancer activities. On the other hand, pharmacological properties of benzodiazepines include antianxiety, anticance

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25

Broudic, Nathan, Alexandra Pacheco-Benichou, Cécile Corbière, et al. "Novel Thiazole-Fused [4,5-g] or [5,4-g]Quinazolin-8-ones and Their Quinazoline Analogues: Synthesis and Biological Evaluation." Pharmaceuticals 17, no. 11 (2024): 1452. http://dx.doi.org/10.3390/ph17111452.

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Background/Objectives: In connection with previous work on V-shaped polycyclic thiazolo[5,4-f]quinazolin-9-one and [5,4-f]quinazoline derivatives that can modulate the activity of various kinases, the synthesis of straight thiazole-fused [4,5-g] or [5,4-g]quinazolin-8-ones and quinazoline derivatives hitherto undescribed was envisioned. Methods: An innovative protocol allowed to obtain the target structures. The synthesis of inverted thiazolo[4,5-h] and [5,4-h]quinazolin-8-one derivatives was also explored with the aim of comparing biological results. The compounds obtained were tested against

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Osarumwense, P. O., M. O. Edema, and C. O. Usifoh. "Synthesis And Anagesic activities of Quinazolin-4(3H)-One, 2-Methyl-4(3H)-Quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one." Journal of Drug Delivery and Therapeutics 10, no. 4-s (2020): 87–91. http://dx.doi.org/10.22270/jddt.v10i4-s.4209.

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Background: Objective: The current 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 analgesic activity. Method: The condensation of 2-amino-methyl-4-methoxybenzoate with acetic anhydride yielded the cyclic compound 2-methyl-4, 5-disubstituted-1, 3-benzo-oxazine-4-one which further 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–Ph

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27

Krasovska, Nataliia, Viktor Stavytskyi, Inna Nosulenko, Oleksandr Karpenko, Oleksii Voskoboinik, and Serhii Kovalenko. "Quinazoline-containing Hydrazydes of Dicarboxylic Acids and Products of Their Structural Modification: A Novel Class of Anti-inflammatory Agents." Acta Chimica Slovenica 68, no. 2 (2021): 395–403. http://dx.doi.org/10.17344/acsi.2020.6440.

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The synthesis of hydrazides formed by quinazolin-4(3H)-ylidenehydrazine and dicarboxylic acids, as well as their further modification are described in the present manuscript. It was shown that above-mentioned hydrazides may be obtained via acylation of initial quinazolin-4(3H)-ylidenehydrazine by corresponding acylhalides, cyclic anhydrides and imidazolides of dicarboxylic acids monoesters. Obtained hydrazides were converted into [1,2,4]triazolo[1,5-с]quinazolines that were used as initial compounds for chemical modification aimed to the introduction of amide fragment to the molecule. The IR,

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28

Ning, Weiwei, Ju Zhu, Canhui Zheng, et al. "Fragment-Based Design of Novel Quinazolinon Derivatives as Human Acrosin Inhibitors." Chemical Biology & Drug Design 81, no. 4 (2013): 437–41. http://dx.doi.org/10.1111/cbdd.12106.

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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 performe

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30

Nerkar, Amit G. "Medicinal chemistry of some marketed quinazolin/-es/-ones as medicines." Current Trends in Pharmacy and Pharmaceutical Chemistry 5, no. 4 (2023): 109–13. http://dx.doi.org/10.18231/j.ctppc.2023.025.

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Quinazolinone nucleus has wide applications in medicine. This editorial gives a detailed account of some marketed quinazolinones along with medicinal chemistry for medicinal chemistry aspect of quinazolinones. The editorial includes some marketed, some withdrawn from market and most FDA approved quinazolinones as medicines.

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31

Amrutkar, Rakesh D., Sunil V. Amrutkar, and Mahendrasing S. Ranawat. "Quinazolin-4-One: A Varsatile Molecule." Current Bioactive Compounds 16, no. 4 (2020): 370–82. http://dx.doi.org/10.2174/1573407215666181120115313.

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Background:Quinazolines and quinazolinones constitute a major class of biologically active molecules both from natural and synthetic sources. We will limit this review to compounds possessing the 4(3H)-quinazolinone skeleton, which is found in compounds displaying significant biological and pharmacological properties. The molecular design of potential lead compound is still a key line of approach for the discovery and development of new chemical entities. A combination of two or more chemical moieties into one is a common approach of operation and this can most likely result in the improvement

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Marinho, Elina, and M. Fernanda Proença. "Acid catalyzed synthesis of 2-(2-aminophenyl)quinazoline-4-amine and reaction with aromatic aldehydes." RSC Advances 6, no. 8 (2016): 6138–43. http://dx.doi.org/10.1039/c5ra19785f.

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The hydrochloride salt of 2-(2-aminophenyl)quinazoline-4-amine, prepared from a quinazolino[3,4-a]quinazoline, was reacted with aromatic aldehydes under conventional heating or microwave irradiation, leading to tetracyclic dihydroquinazolines.

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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 CO

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Molina, Pedro, Mateo Alajarín, and Angel Vidal. "New methodology for the preparation of quinazoline derivatives via tandem aza-wittig/heterocumulene-mediated annulation. Synthesis of 4(3H)-quinazolinones, benzimidazo[1,2-c] quinazolines, quinazolino[3,2-a]quinazolines and benzothiazolo[3,2-c]quinazolines." Tetrahedron 45, no. 13 (1989): 4263–86. http://dx.doi.org/10.1016/s0040-4020(01)81321-1.

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Jalani, Hitesh B., Jitendra C. Kaila, Arshi B. Baraiya, Amit N. Pandya, V. Sudarsanam, and Kamala K. Vasu. "A versatile one-pot multicomponent synthesis of novel quinazolinon-2-yl-tetrasubstituted thiophenes." Tetrahedron Letters 51, no. 43 (2010): 5686–89. http://dx.doi.org/10.1016/j.tetlet.2010.08.046.

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Auti, Prashant S., Ginson George, and Atish T. Paul. "Recent advances in the pharmacological diversification of quinazoline/quinazolinone hybrids." RSC Advances 10, no. 68 (2020): 41353–92. http://dx.doi.org/10.1039/d0ra06642g.

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Deharkar, Pravin, Shridhar Satpute, and Deepa Panhekar. "Review on Synthesis Route of Quinazoline Based Hybrid Derivatives." Asian Journal of Chemistry 33, no. 11 (2021): 2525–47. http://dx.doi.org/10.14233/ajchem.2021.23373.

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Quinazolines are amidst the most significant pharmacological compounds in natural and medicinal chemistry, with a wide variety of pharmacological things, including antifungal, antibacterial, anti-inflammatory, anti-HIV, anticancer and analgesic activity. Designing innovative quinazolines, studying possible techniques to synthesize quinazolines, examining diverse features of quinazolines and looking for prospective uses of quinazolines have all become more important in the last two decades due to their multiple possible applications. The current review paper discusses the synthesis of quinazoli

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Lipunova, Galina N., Emiliya V. Nosova, Valery N. Charushin, and Oleg N. Chupakhin. "Functionalized Quinazolines and Pyrimidines for Optoelectronic Materials." Current Organic Synthesis 15, no. 6 (2018): 793–814. http://dx.doi.org/10.2174/1570179415666180622123434.

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Background: Quinazolines, the important group of benzodiazines, are widely known in medicinal chemistry due to their broad spectrum of biological activities. Notably, extensive research on the synthesis and application of quinazoline derivatives for electronic devices, luminescent elements, photoelectric conversion elements, and image sensors has been published recently. Objective: This review reports luminescent small molecules and chelate compounds including a quinazoline or pyrimidine ring in their scaffold highlighting their applications related to photo- and electroluminescence. Conclusio

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Debnath, Subal, and S. Y. Manjunath. "Conventional and Microwave Assisted Synthesis of 3-(Substituted)-2-phenyl quinazolin-4(3H)-one and their Antibacterial and Anthelmintic Activity." International Journal of Pharmaceutical Sciences and Nanotechnology 4, no. 2 (2011): 1408–11. http://dx.doi.org/10.37285/ijpsn.2011.4.2.6.

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The present research work was aimed to synthesize a series of various substituted quinazolinone containing 3-(substituted)-2-phenylquinazolin-4(3H)-one. The compound 3-[(2-oxo-4-phenylazetidin-1-yl)-carbonyl]-2-phenylquinazolin-4(3H)-one, II was prepared by treating 4-oxo-2-phenyl-N-[(E)-phenylmethylidene]quinazoline-3(4H)-carboxamide, I with acetyl chloride and triethylamine (TEA) in benzene by conventional and microwave irradiation method. Synthesis of 3-[{2-oxo-3-(2,4-dichlorophenoxy)-4-phenylazetidin-carbonyl]-2-phenylquinazolin-4(3H)-one, III was carried out by reacting, I with 2,4-dichlo

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Paduri Karunakar, Swetha Gujjewar, Somesh Sharma, et al. "Design, Synthesis and Anticancer activity of novel Triazole substituted Quinazoline Hybrids." International Journal of Research in Pharmaceutical Sciences 11, no. 3 (2020): 3569–79. http://dx.doi.org/10.26452/ijrps.v11i3.2513.

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Quinazolines and 1,2,4-triazoles are important class of nitrogen containing heterocyclic compounds having immense biological importance. From the literature review, pharmacokinetic properties of a drug can be modified or enhanced by building a triazole moiety into a compound like quinazoline. Therefore, the study of new hybrid systems which combines triazole system with quinazoline is still seemed warranted. In the present study, a sequence of novel 1,2,4-triazole derivatives containing quinazolinyl moiety were designed, synthesized and screened for their in vitro anticancer activity. Thirteen

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Vaskevych, Alla, Nataliia Savinchuk, and Mykhailo Vov. "Synthesis of pyrrolo(pyrido)[1,2-a]quinazolinones and their benzoannulated analogues: An overview." Current Chemistry Letters 14, no. 3 (2025): 507–32. https://doi.org/10.5267/j.ccl.2025.3.005.

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Angular pyrrolo(pyrido)[1,2-a]quinazolinones, being structurally isomeric to linear pyrrolo(pyrido)[2,1-b]quinazolinone alkaloids, are attractive molecular systems for both synthetic transformations and targeted biomedical research. The pyrrolo(pyrido)[1,2-a]quinazolinone scaffold has proven to be quite effective in the search for compounds with a wide range of pharmacological activities, e.g. anti-inflammatory, antioxidant, antibacterial, antiarrhythmic, and inhibitors of important biotargets. The present review summarises the methods for the synthesis of pyrrolo(pyrido)[1,2-a]quinazolinones

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Zhang, Zhe, Min Wang, Chaofeng Zhang, Zhixin Zhang, Jianmin Lu та Feng Wang. "The cascade synthesis of quinazolinones and quinazolines using an α-MnO2 catalyst and tert-butyl hydroperoxide (TBHP) as an oxidant". Chemical Communications 51, № 44 (2015): 9205–7. http://dx.doi.org/10.1039/c5cc02785c.

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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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Pozharskii, Alexander F., Valery A. Ozeryanskii, Vladimir Y. Mikshiev, Anatoly V. Chernyshev, Anatoly V. Metelitsa та Alexander S. Antonov. "Proton-induced fluorescence in modified quino[7,8-h]quinolines: dual sensing for protons and π-donors". Organic & Biomolecular Chemistry 17, № 35 (2019): 8221–33. http://dx.doi.org/10.1039/c9ob01391a.

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Abdel-Megeed, Mohamed Farghali, and Abderrahman Teniou. "Synthesis of some 3-substituted 4(3H)-quinazolinone and 4(3H)-quinazolinethione derivatives and related fused biheterocyclic ring systems." Collection of Czechoslovak Chemical Communications 53, no. 2 (1988): 329–35. http://dx.doi.org/10.1135/cccc19880329.

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The reactions of 2-phenyl-4(3H)-quinazoline, 2-phenyl-3-amino-4(3H)-quinazolinone, and corresponding thiones with phenyl isocyanate or phenyl isothiocyanate were investigated. The resulting urea and thiourea quinazolinone or quinazolinethione derivatives reacted with hydrazine hydrate, phenylhydrazine, and urea or thiourea to form fused biheterocyclic ring systems with potential biological activities. The products were identified by IR, 1H NMR, and mass spectroscopy.

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Santagati, Andrea, Maria Modica, Luigi Monsù Scolaro, and Maria Santagati. "New Synthetic Approaches to Fused Heterocyclo-quinazolines." Journal of Chemical Research 23, no. 2 (1999): 86–87. http://dx.doi.org/10.1177/174751989902300210.

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Fused heterocyclo-quinazolines have been prepared from the versatile and easily obtained intermediate 3-amino-2,3-dihydro-2-thioxo-4(1 H)-quinazolinone 2; their structural elucidation is also reported.

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47

Wang, Wang, Pei-Sen Zou, Li Pang, et al. "Synthesis of spiroindolenine-3,3′-pyrrolo[2,1-b]quinazolinones through gold(i)-catalyzed dearomative cyclization of N-alkynyl quinazolinone-tethered indoles." Organic & Biomolecular Chemistry 20, no. 10 (2022): 2069–74. http://dx.doi.org/10.1039/d1ob02492b.

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An efficient gold(i)-catalyzed dearomative cyclization of N-alkynyl quinazolinone-tethered C2-substituted indoles to prepare various spiroindolenine-3,3′-pyrrolo[2,1-b]quinazolinones in good to excellent yields is reported.

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48

Wang, Hengshuai, Shengchao Jiao, Kerong Chen, et al. "Direct access to pyrido/pyrrolo[2,1-b]quinazolin-9(1H)-ones through silver-mediated intramolecular alkyne hydroamination reactions." Beilstein Journal of Organic Chemistry 11 (March 30, 2015): 416–24. http://dx.doi.org/10.3762/bjoc.11.47.

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We report a synthetic methodology for the construction of the fused heterocyclic compounds pyrido[2,1-b]quinazolin-9(1H)-ones and pyrrolo[2,1-b]quinazolin-9(1H)-ones through an AgOTf-catalyzed intramolecular alkyne hydroamination reaction. The methodology is applicable to a wide scope of substrates and produces a series of fused quinazolinone heterocycles in good to excellent yields.

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Patel, Harun, Rahul Pawara, and Sanjay Surana. "Resolving the Mystery of Ring Opening in the Synthesis of Benzo[d][1, 3]oxazin-4-one and Quinazolin-4(3H)-one." Letters in Organic Chemistry 16, no. 11 (2019): 898–905. http://dx.doi.org/10.2174/1570178616666181217114030.

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Quinazoline is the six-membered heterocyclic ring system reported for its versatile biological activities. This characteristic feature of quinazoline makes it a good template for a lead generation library. Ring opening is one of the major concerns in the synthesis of quinazolin-4(3H)-one that results in diamide formation. Here, alternative fusion strategy is reported, which is a time-saving and costeffective method to overcome the ring opening problem associated with the synthesis of benzo[ d][1,3]oxazin-4-one and quinazolin-4(3H)-one.

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C. O., Usifoh, and Ukoh G. C. "Triflate-mediated Synthesis of 3-(4-Methoxyquinazolin-2-yl)- quinazolin-2,4-(1H,3H)-dione and its Antimicrobial Activity." Scientia Pharmaceutica 70, no. 2 (2002): 123–28. http://dx.doi.org/10.3797/scipharm.aut-02-14.

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The synthesis of a novel quinazolinone was accomplished by the reaction of quinazolin- 2,4-(1H,3H)-dione with trifluoromethanesulfonic anhydride in triethylamine. The antimicrobial activity was determined against eight microorganisms. The organisms were all susceptible to 3-(4-methoxyquinazolin-2-yl)-quinazolin-2,4-(1H,3H)-dione 3 at the concentrations used. The gram positive organisms showed more susceptibility than the gram negative ones.

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