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Journal articles on the topic 'Quinazolinone derivatives'

Author: Grafiati

Published: 4 June 2025

Last updated: 1 August 2025

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1

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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2

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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3

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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4

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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5

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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6

Prakash, Gaurav, Ajay Kumar Das, and V. D. Tripathi. "A Catalyst Free and Sustainable Synthesis of Quinazolinones in Glycerol as Green Solvent." Asian Journal of Chemistry 35, no. 5 (2023): 1089–94. http://dx.doi.org/10.14233/ajchem.2023.27612.

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In this article, glycerol was employed in a quest to develop an environmentally benign and sustainable synthetic protocol for synthesis of quinazolinone and spiro-quinazolinone derivatives. These studies were performed to investigate the effect of electron-rich and electronegative groups on the synthetic route of an established protocol. Different substituted isatin and benzaldehyde derivatives have been incorporated to synthesize analogues of two series of quinazolinones in order to investigate the efficacy of the developed methodology and substrate tolerance. A total of 12 derivatives were s

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7

Mishra, AD. "A New Route for the Synthesis of Quinazolinones." Nepal Journal of Science and Technology 12 (July 22, 2012): 133–38. http://dx.doi.org/10.3126/njst.v12i0.6491.

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Quinazolinone derivatives are highly bioactive heterocyclic compounds with wider range of microbial activities such as anti-malarial, anti-cancer, anti-inflammatory, anti-hypertensive, anti-convulsant, anti-HIV, etc. Solid supported microwave synthesis of some 3-substituted-4-(2H)-quinazolinones has been carried out by the reaction of anthranilic acid, formaldehyde and primary aromatic amines. The usage of hazardous reagents and organic solvents has been avoided. The reactions were conducted in presence of acidic alumina where formaldehyde entered into cycloaddition to yield the quinazolinone

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8

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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9

Yaduwanshi, Phool Singh, Sheelu Singh, Prinsi Sahapuriya, Priyanka Dubey, Jyoti Thakur, and Savita Yadav. "Synthesis of Some Noval Qunazolinone Derivatives for their Anticonvulsant Activity." Oriental Journal Of Chemistry 40, no. 2 (2024): 369–73. http://dx.doi.org/10.13005/ojc/400207.

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The quinoline family comprises an appealing group of heterocyclic compounds, with quinazolinones and their synthetic analogs being of particular interest. To synthesize 3- amino 2-phenyl quinazolinones, anthranilic acid and its substituted derivatives were employed as initial materials. The MES method was utilized to evaluate the anticonvulsant activity of the developed substances on albino mice, with phenytoin serving as a benchmark anticonvulsant medication.The synthesized compounds demonstrated noteworthy anticonvulsant activity, comparable to that of established prescription medications. A

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10

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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11

Niharika, P., J. Risy Namratha, N. Sunitha, and S. Manohar Babu. "Synthesis and evaluation of 6-Fluoro benzothiazole substituted quinazolinones." Current Trends in Pharmacy and Pharmaceutical Chemistry 4, no. 1 (2022): 35–40. http://dx.doi.org/10.18231/j.ctppc.2022.007.

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The present work was hypothesized to synthesize Benzothiazole substituted diethyl amino Quinazolinone derivatives and evaluate their antimicrobial activity. Quinazolinones were synthesized from condensation of 2-amino benzothiazole, anthranilic acid and acetic anhydride further followed by condensation with formaldehyde and diethyl amine. Antimicrobial activity was evaluated by agar disc diffusion using organisms and anti-inflammatory and antioxidant activies were studied using albumin denaturation and hydrogen peroxide radical scavenging methods. The structures of the synthesized Quinazolinon

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12

Gong, Tang, Liu та Liu. "Synthesis and Evaluation of Novel 2H-Benzo[e]-[1,2,4]thiadiazine 1,1-Dioxide Derivatives as PI3Kδ Inhibitors". Molecules 24, № 23 (2019): 4299. http://dx.doi.org/10.3390/molecules24234299.

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In previous work, we applied the rotation-limiting strategy and introduced a substituent at the 3-position of the pyrazolo [3,4-d]pyrimidin-4-amine as the affinity element to interact with the deeper hydrophobic pocket, discovered a series of novel quinazolinones as potent PI3Kδ inhibitors. Among them, the indole derivative 3 is one of the most selective PI3Kδ inhibitors and the 3,4-dimethoxyphenyl derivative 4 is a potent and selective dual PI3Kδ/γ inhibitor. In this study, we replaced the carbonyl group in the quinazolinone core with a sulfonyl group, designed a series of novel 2H-benzo[e][1

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13

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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14

Salahuddin, Nehal, Ahmed A. Elbarbary, and Hend A. Alkabes. "Quinazolinone Derivatives Loaded Polypyrrole/Chitosan Core–Shell Nanoparticles with Different Morphologies: Antibacterial and Anticancer Activities." Nano 12, no. 01 (2017): 1750002. http://dx.doi.org/10.1142/s1793292017500023.

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Polypyrrole/chitosan (PPC) spherical dark nanoparticles surrounded by shadow spheres were fabricated through in situ oxidative polymerization of pyrrole in presence of chitosan (CS) using ferric chloride (FeCl3) as oxidant and evaluated as a carrier for some amino-quinazolinone derivatives (I–IV). The loading of amino-quinazolinone derivatives (I–IV) into the core–shell nanoparticles were investigated by thermal gravimetric analysis (TGA). Quinazolinone derivatives (I–IV) loaded nanoparticles showed inter-connected sphere in necklace-like morphology, rods or filaments depending on the function

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15

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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16

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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17

Fišnerová, Ludmila, Bohumila Brunová, Zuzana Kocfeldová, Jana Tíkalová, Eva Maturová, and Jaroslava Grimová. "Synthesis and analgetic efficiency of some oxy and oxo derivatives of 4(3H)-quinazolinone." Collection of Czechoslovak Chemical Communications 56, no. 11 (1991): 2373–81. http://dx.doi.org/10.1135/cccc19912373.

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A series of 3-substituted 4(3H)-quinazolinone derivatives have been prepared by alkylation of 4(3H)-quinazolinone with halogenoethers, halogenoketones, and Mannich bases, and the products have been tested for analgetic effects.The most interesting representatives of the oxy and oxo derivatives are 3-[2-(2’,4’-difluoro-4-biphenylyloxy)ethyl]-4(3H)-quinazolinone (Ib) and 3-[2-oxo-2-(4-biphenylyl)ethyl]-4(3H)-quinazolinone (IIi), respectively. Among the group of oxy derivatives also the 2-methylderivative Ig has been prepared, viz. by alkylation of 2’,4’-difluoro-4-hydroxybiphenyl with 2-methyl-3

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18

Abdou, Ibrahim M., and Shaikha S. Al-Neyadi. "Synthesis of quinazolines and quinazolinones via palladium-mediated approach." Heterocyclic Communications 21, no. 3 (2015): 115–32. http://dx.doi.org/10.1515/hc-2014-0181.

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AbstractQuinazoline derivatives have drawn attention in the field of heterocyclic chemistry because of their unique skeleton and interesting biological applications. This review summarizes the recent palladium-catalyzed reactions used to construct quinazoline and its related 4(3H)-quinazolinone analogues. The mechanisms of some Pd-catalyzed reactions are also discussed.

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19

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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20

Bollini, Mariela, Ana M. Bruno, María E. Niño, et al. "Synthesis, 2D-QSAR Studies and Biological Evaluation of Quinazoline Derivatives as Potent Anti-Trypanosoma cruzi Agents." Medicinal Chemistry 15, no. 3 (2019): 265–76. http://dx.doi.org/10.2174/1573406414666181005145042.

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Background: Chagas disease affects about 7 million people worldwide. Only two drugs are currently available for the treatment for this parasite disease, namely, benznidazol (Bzn) and nifurtimox (Nfx). Both drugs have limited curative power in the chronic phase of the disease. Therefore, continuous research is an urgent need so as to discover novel therapeutic alternatives. Objective: The development of safer and more efficient therapeutic anti-T. cruzi drugs continues to be a major goal in trypanocidal chemotherapy. Method: Synthesis, 2D-QSAR and drug-like physicochemical properties of a set o

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21

Widiyana, Anita Puspa, Galih Satrio Putra, Luthfi Ahmad Muchlashi, Mellany Ika Sulistyowaty, and Tutuk Budiati. "Design and Molecular Docking Studies of Quinazoline Derivatives as Antiproliferation." JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA 3, no. 2 (2018): 44. http://dx.doi.org/10.20473/jfiki.v3i22016.44-48.

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Background: Nowadays, a lot of new active substances as anticancer agents have been developed. One of the protein targets of anticancer is selective cyclooxygenase-2 (COX-2). Selective COX-2 is the regulator of cell proliferation. Objective: In this research, quinazoline derivatives were used to design the anticancer agent through a selective COX-2 inhibition. The potential activity of quinazoline derivatives could be increased by substitution in position 2 and 3 of quinazolinone. Molecular docking of selective COX-2 inhibition was required to predict their antiproliferation activity. Methods:

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Deshmukh, M. B., and Savita Dhongade (Desai). "Synthesis and QSAR Study of Some HDL Cholesterol Increasing Quinazolinone Derivatives." E-Journal of Chemistry 1, no. 1 (2004): 17–31. http://dx.doi.org/10.1155/2004/671567.

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We describe here an easy and efficient method to obtainS-alkylated derivatives of thio-quinazolinone using different alkylating agents via a solvent-free microwave-assisted method. The alkylated thio quinazolinones were further sequentially condensed with hydrazine hydrate and different aromatic aldehydes to get the hydrazones, which were studied for QSAR. The synthesized compounds were subjected to a prediction of biological activities. A software application (PASS) was used for this purpose. The relationship between structure and different biological activities was studied and the different

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Nerkar, A. G., A. K. Saxena, S. A. Ghone, and A. K. Thaker. "In SilicoScreening, Synthesis andIn VitroEvaluation of Some Quinazolinone and Pyridine Derivatives as Dihydrofolate Reductase Inhibitors for Anticancer Activity." E-Journal of Chemistry 6, s1 (2009): S97—S102. http://dx.doi.org/10.1155/2009/506576.

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Dihydrofolate reductase (DHFR) is the important target for anticancer drugs belonging to the class of antimetabolites as the enzyme plays important role in the de novo purine synthesis. We here report thein silicoscreening to obtain best fit molecules as DHFR inhibitors, synthesis of some ʻbest fitʼ quinazolinone from 2-phenyl-3-(substituted-benzilidine-amino) quinazolinones (Quinazolinone Shiff's bases) QSB1-5and pyridine-4-carbohydrazide Shiff's bases (ISB1-5) derivatives and theirin vitroanticancer assay. Synthesis of the molecules was performed using microwave assisted synthesis. The struc

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El-Sayed, Amira A., Mahmoud F. Ismail, Abd El-Galil E. Amr, and Ahmed M. Naglah. "Synthesis, Antiproliferative, and Antioxidant Evaluation of 2-Pentylquinazolin-4(3H)-one(thione) Derivatives with DFT Study." Molecules 24, no. 20 (2019): 3787. http://dx.doi.org/10.3390/molecules24203787.

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The current study was chiefly designed to examine the antiproliferative and antioxidant activities of some novel quinazolinone(thione) derivatives 6–14. The present work focused on two main points; firstly, comparing between quinazolinone and quinazolinthione derivatives. Whereas, antiproliferative (against two cell lines namely, HepG2 and MCF-7) and antioxidant (by two methods; ABTS and DPPH) activities of the investigated compounds, the best quinazolinthione derivatives were 6 and 14, which exhibited excellent potencies comparable to quinazolinone derivatives 5 and 9, respectively. Secondly,

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Ghosh, Suman Kr, and Rajagopal Nagarajan. "NIS-mediated regioselective amidation of indole with quinazolinone and pyrimidone." RSC Adv. 4, no. 39 (2014): 20136–44. http://dx.doi.org/10.1039/c4ra02417f.

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A mild, metal-free condition was developed for the direct regioselective C2 amidation of indoles and pyrroles with quinazolinone and pyrimidone derivatives in intermolecular fashion, which led to novel indolyl/pyrrolyl quinazolinone and pyrimidone derivatives in moderate to good yields.

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B. Deshmukh, M., and Savita Dhongade (Desai). "Synthesis and QSAR Study of (4-Oxo-3-aryl-3,4-dihydro-quinazolin-2-ylsulfanyl)-propionic Acid arylidene/aryl-ethylidene-hydrazides via Microwave Assisted Solvent Free Reations." E-Journal of Chemistry 1, no. 2 (2004): 115–26. http://dx.doi.org/10.1155/2004/142148.

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In the present work,s-alkylated derivatives of thio-quinazolinone were obtained using Methyl 2-chloro propionate via a solvent-free microwave-assisted method. The alkylated thio quinazolinones were further sequentially condensed with hydrazine hydrate and different aromatic aldehydes to get the hydrazides, which were studied for QSAR. The synthesized compounds were subjected to a prediction of biological activities. A software application (PASS) was used for this purpose. . The relationship between structure and different biological activities was studied and the different derivatives were rec

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27

Ritik R. Jamgade, Ritik R. Jamgade, Dr Dinesh R. Chaple Dr. Dinesh R. Chaple, Rida K. Saiyyad Rida K. Saiyyad, Prerna P. Bhange Prerna P. Bhange, Nandani K. Sonwane Nandani K. Sonwane, and Shivani P. Wadichar Shivani P. Wadichar. "Molecular Docking and ADME-Based Prioritization of 20 Quinazolinone Scaffolds for Anticonvulsant Potential." International Journal of Pharmaceutical Research and Applications 10, no. 3 (2025): 2046–63. https://doi.org/10.35629/4494-100320462063.

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Quinazolinone derivatives have attracted significant attention for their broad pharmacological potential, particularly in the treatment of central nervous system (CNS) disorders such as epilepsy. In the present study, a series of twenty novel quinazolinone derivatives were designed and evaluated for their potential anticonvulsant activity through molecular docking studies. The compounds were docked into the active site of the GABAAreceptor, a wellestablished target for antiepileptic drugs, using its crystallographic structure (PDB ID: 4COF). Molecular docking was carried out using AutoDockVina

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Starikova, Alla, Marina Samotrueva, Natalia Zolotareva, Daria Merezhkina, and Aleksandr Ozerov. "STUDY OF THE RELATIONSHIP BETWEEN THE ANTIMICROBIAL AND HYPOGLYCAEMIC ACTIVITIES OF NEW QUINAZOLINONES BY MATHEMATICAL MODELLING." CASPIANJOURNALOF MEDICINE AND PHARMACY 4, no. 1 (2023): 63–70. http://dx.doi.org/10.29039/2712-8164-2023-1-63-70.

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To date, quinazolinone derivatives, which have a unique chemical structure and exhibit a wide range of pharmacological activity, are used both as drugs and starting substances in the synthesis of deriva-tives with multitarget activity. Quinazolinones synthesized by the scientists of Volgograd Medical Uni-versity are characterized by the pronounced antimicrobial activity against Staphylococcus aureus, Streptococcus pneumoniae, Escherichia coli, Klebsiella. Computer-assisted prediction of the pharma-cological action spectrum by the PASS programme of the studied quinazolinone derivatives shows a

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Mahmoud, Mahmoud R., Eman A. A. El-Bordany, Naglaa F. Hassan, and Fatma S. M. Abu El-Azm. "New 2,3-Disubstituted Quinazolin-4(3H)-Ones from 2-Undecyl-3,1-Benzoxazin-4-One." Journal of Chemical Research 2007, no. 9 (2007): 541–44. http://dx.doi.org/10.3184/030823407x248315.

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2-undecyl-4H-3,1-benzoxazin-4-one (2) was prepared and reacted with primary and secondary amines affording compounds 3–7, while with hydrazine hydrate it gave the quinazolinone derivative 8. The reaction of 8 with 3,4,5-trimethoxybenzaldehyde followed by thioglycollic acid yielded 9 and 10, respectively. Acylation of 8 using cinnamoyl chloride gave 11. Furthermore, treatment of 2 with hydrazine derivatives provided 12 and 13. Fusion of 2 with ammonium acetate gave the quinazolinone derivative 14 which upon treatment with ethyl chloroacetate yielded the ester 15. The hydrazide 17 was obtained f

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Aravind, A*. "Quinazoline Based Dual Inhibitors of EGFR and VEGFR as Potential Anti-proliferative Agents-A Review." International Journal of Pharmacy and Biological Sciences (IJPBS) 14, no. 4 (2024): 1–12. https://doi.org/10.5281/zenodo.14168646.

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AbstractIt has been established that the overexpression of tyrosine kinase inhibitors, EGFR and VEGFR is the primary factor contributing to the development and spread of carcinomas, including pancreatic, lung, and breast cancers. Quinazoline nucleus is a distinct and flexible scaffold with a broad range of pharmacological action, particularly in the area of tyrosine kinase inhibitors, where the US Food and Drug Administration has approved more than twenty small molecule inhibitors in the past 20 years. Quinazoline derivatives are effective inhibitors of EGFR and VEGFR, which are key targets in

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Masri, Abdulkader, Ayaz Anwar, Naveed Ahmed Khan, et al. "Antibacterial Effects of Quinazolin-4(3H)-One Functionalized-Conjugated Silver Nanoparticles." Antibiotics 8, no. 4 (2019): 179. http://dx.doi.org/10.3390/antibiotics8040179.

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Infections due to multi-drug resistant bacteria are on the rise and there is an urgent need to develop new antibacterials. In this regard, a series of six functionally diverse new quinazolinone compounds were synthesized by a facile one-pot reaction of benzoic acid derivatives, trimethoxymethane and aniline derivatives. Three compounds of 3-aryl-8-methylquinazolin-4(3H)-one, and 3-aryl-6,7-dimethoxyquinazolin4(3H)-one were prepared and tested against multi-drug resistant bacteria. Furthermore, we determined whether conjugation with silver nanoparticles improved the antibacterial efficacy of th

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Lin, Wei, Qun Zhao, Yao Li, et al. "Asymmetric synthesis of N–N axially chiral compounds via organocatalytic atroposelective N-acylation." Chemical Science 13, no. 1 (2022): 141–48. http://dx.doi.org/10.1039/d1sc05360d.

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A highly efficient atroposelective N-acylation reaction of quinazolinone type benzamides with cinnamic anhydrides for the direct catalytic synthesis of optically active atropisomeric quinazolinone derivatives was developed.

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Yadav, Meena K., Laxmi Tripathi, and Diptendu Goswami. "SYNTHESIS AND ANTICONVULSANT ACTIVITY (CHEMO SHOCK) OF N-1(SUBSTITUTED-N-4[(4-OXO-3-PHENYL-3, 4-DIHYDRO-QUINAZOLINE-2-YLMETHYL) SEMICARBAZONES." Asian Journal of Pharmaceutical and Clinical Research 10, no. 4 (2017): 359. http://dx.doi.org/10.22159/ajpcr.2017.v10i4.16876.

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Objective: This work is designed at finding new structure leads with potential anticonvulsant activities of 4(3H)-quinazolinone pharmacophore scaffold.Methods: A new series of 4(3H)-quinazolinone pharmacophore was designed with substituted moieties possesses different electronic environment in the hope of developing potent and safe new effective compounds. In such fashion, in this paper, we report the synthesis and anticonvulsant activity (Chemo shock) of N-1(substituted-N-4[(4-oxo-3-phenyl-3, 4-dihydro-quinazoline-2-ylmethyl) semicarbazones 3A-d (1-7), 3B-d (1-7), 3C-d (1-7), their chemical s

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34

Doan Thi Yen, Oanh, Binh Vo Ngoc, and Anh Ngo Quoc. "SODIUM SULFIDE-PROMOTED REACTION OF 2-AMINOBENZAMIDE AND BENZYL ALCOHOLS WITH ELEMENTAL SULFUR: A NOVEL APPROACH WITH 2-ARYL-QUINAZOLIN-4(3H)." Journal of Science Natural Science 67, no. 3 (2022): 83–89. http://dx.doi.org/10.18173/2354-1059.2022-0044.

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A simple metal- and solvent-free method for the synthesis of 2-aryl- 4(3H)-quinazolinone derivatives from 2-aminobenzamide and benzyl alcohols in the presence of S8\DMSO as an oxidizing agent and promoted by Na2S.5H2O has been reported. Five 2-aryl-4(3H)-quinazolinone derivatives were synthesized with yields from 23% to 86%.

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Vijayakumar, K., A. Jafar Ahamed, and G. Thiruneelakandan. "Synthesis, Antimicrobial, and Anti-HIV1 Activity of Quinazoline-4(3H)-one Derivatives." Journal of Applied Chemistry 2013 (September 12, 2013): 1–5. http://dx.doi.org/10.1155/2013/387191.

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The present investigation aims to synthesize 11 compounds of quinazoline-1 derivatives and to test their antimicrobial and anti-HIV1 activities. A quick-witted method was developed for the synthesis of novel substituted quinazolinone derivatives by summarizing diverse diamines with benzoxazine reactions, and it demonstrated the benefits of typical reactions, handy operation, and outstanding product yields. These compounds were confirmed by elemental analysis, I R, 1H NMR, 13C NMR, and mass spectra. Then antimicrobial and anti-HIV1 activities of the compounds were tested in-vitro. It was found

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Hashem, Heba E., and Ahmed M. Abo-Bakr. "Synthesis of Some New 1,2,4-Triazine and 1,2,5-Oxadiazine Derivatives with Antimicrobial Activity." Heteroatom Chemistry 2019 (September 25, 2019): 1–7. http://dx.doi.org/10.1155/2019/2326514.

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1,2,4-Triazine and 1,2,5-oxadiazine derivatives 2–12 were obtained from treated 1,3-oxazolone (1) with phenyl hydrazine or hydroxylamine hydrochloride. Chlorotriazine derivative 3 undergoing condensation reactions with different reagents produced new fused tetrazolo-triazine and triazino-quinazolinone derivatives. 1,2,5-Oxadiazine has been used as a synthon for the fused pyrazolo-oxadiazine derivative. The constitution of the prepared compounds was built up based on microanalytical and spectral data. Some of the new compounds were assessed for their antimicrobial activity.

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Smith, Keith, Gamal A. El-Hiti, Mohamed F. Abdel-Megeed, and Mohamed A. Abdo. "Convenient Synthesis of More Complex 2-Substituted 4(3H)-Quinazolinones via Lithiation of 2-Alkyl-4(3H)-quinazolinones." Collection of Czechoslovak Chemical Communications 64, no. 3 (1999): 515–26. http://dx.doi.org/10.1135/cccc19990515.

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2-Methylquinazolin-4(3H)-one has been doubly lithiated, at nitrogen and in the 2-methyl group, with n-butylithium. The lithium reagent thus obtained reacts with a variety of electrophiles (iodomethane, D2O, phenyl isocyanate, benzaldehyde, benzophenone, cyclopentanone, 2-butanone, carvone) to give the corresponding 2-substituted derivatives in very good yields. Reaction of the dilithio reagent with acetonitrile gives an α,β-unsaturated imine by tautomerization of the initial addition product. Double lithiation of 2-ethyl- and 2-propyl-4(3H)-quinazolinones can be achieved using lithium diisopro

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Ghosh, Prasanjit, Bhaskar Ganguly, and Sajal Das. "C–H functionalization of quinazolinones by transition metal catalysis." Organic & Biomolecular Chemistry 18, no. 24 (2020): 4497–518. http://dx.doi.org/10.1039/d0ob00742k.

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Quinazolinone and its derivatives are an important class of heterocyclic scaffolds in pharmaceuticals and natural products. This review provides the recent research advances in the transition metal catalyzed selective C–H bond functionalization of quinazolinone.

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El-hashash, Maher A., Amira T. Ali, Rasha A. Hussein, and Wael M. El-Sayed. "Synthesis and Reactivity of 6,8-Dibromo-2-ethyl-4H-benzo[d][1,3]oxazin-4-one Towards Nucleophiles and Electrophiles and Their Anticancer Activity." Anti-Cancer Agents in Medicinal Chemistry 19, no. 4 (2019): 538–45. http://dx.doi.org/10.2174/1871520619666190201145221.

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Background: The genetic heterogeneity of tumor cells and the development of therapy-resistant cancer cells in addition to the high cost necessitate the continuous development of novel targeted therapies. Methods: In this regard, 14 novel benzoxazinone derivatives were synthesized and examined for anticancer activity against two human epithelial cancer cell lines; breast MCF-7 and liver HepG2 cells. 6,8-Dibromo-2- ethyl-4H-benzo[d][1,3]oxazin-4-one was subjected to react with nitrogen nucleophiles to afford quinazolinone derivatives and other related moieties (3-12). Benzoxazinone 2 responds to

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USIFOH, C. O. "3-Propynyl-2-substituted Carboxylic Acid Derivatives of Quinazolinone." Scientia Pharmaceutica 68, no. 3 (2000): 275–79. http://dx.doi.org/10.3797/scipharm.aut-00-25.

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Alkylation of quinazolinone-2-carboxylic acids with propargyl bromide in dimethylformamide in the presence of potassium carbonate afforded 3-prop-2-ynyl quinazolinone-2-substituted carboxylic acid derivatives. Further reaction of 4b-c produced 5b-c, which indicates that N-alkylation occurs before esterification with a propynyl moiety.

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EL-BADRY, Y. A., and S. N. ABDOU. "CONSTRUCTION OF SOME NOVEL BIOCIDAL N-ALKYLATED QUINAZOLINE-4(3H)- ONE DERIVATIVES USING MICROWAVE ACTIVATION." Periódico Tchê Química 15, no. 30 (2018): 463–72. http://dx.doi.org/10.52571/ptq.v15.n30.2018.466_periodico30_pgs_463_472.pdf.

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Microwave-assisted construction of 2-propylquinazolinone1 has been achieved, followed by its subsequent utilities in constructing an attractive series of 2,3-disubstituted functional quinazolinones 2-10. The use of microwave irradiation in performing N-alkylation for the titled quinazolinone 1 was applied as a simple, efficient and eco-friendly green technique. Furthermore, the in vitro antimicrobial screening of the obtained compounds 3-10 has been investigated against four bacterial strains and two fungal strains. The structure of the synthesized molecules was affirmed using analytical and s

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Osarumwense, Peter O. "Analgesic activity of newly synthesized 7-chloro–2–methyl-4H–benzo[d] [1,3]–oxazin–4–one and 3–amino-7-chloro-2–methyl-quinazolin-4(3H)–one." Ovidius University Annals of Chemistry 29, no. 1 (2018): 25–28. http://dx.doi.org/10.2478/auoc-2018-0003.

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Abstract The current study is aimed at the analgesic evaluation of quinazolinone derivatives. The quinazolinone derivatives 7-chloro-2-methyl-4H-benzo[d][1,3]-oxazin-4-one and 3-amino-7-chloro-2-methyl-quinazolin-4(3H)-one were evaluated pharmacologically for their in vivo analgesic activities by acetic acid induced writhing in mice. The compounds exhibited significant analgesic activity in the range of 74.67 - 83.80% in comparison to control.

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M.G., Assy, Abdalha A.A., and Abdel Aziz A.E. "Synthesis and Antimicrobial Evaluation of Some New Benzoxazinone and Quinazolinone Derivatives." JOURNAL OF ADVANCES IN CHEMISTRY 8, no. 1 (2016): 1491–99. http://dx.doi.org/10.24297/jac.v8i1.4030.

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Ring opening reactions of benzoxazinone (2) with nitrogen and oxygen nucleophiles gave the corresponding benzamides (3)&(4) and benzoates (5).Quinazolinone derivatives (6) and (7) were obtained upon treatment of (2) with hydrazine hydrate and/or hydroxylamine hydrochloride.Triazole derivatives (8a – b) were obtained when (2) was subjected to react with semicarbazide and/or thiosemicarbazide respectively. Reaction of (2) with sodium azide gave a mixture of tetrazole derivative (9) and benzoimidazolone derivative (10). The antimicrobial activity of some synthesized compounds was examined aga

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Komar, Mario, Maja Molnar, and Anastazija Konjarević. "Screening of Natural Deep Eutectic Solvents for Green Synthesis of 2-methyl-3-substituted Quinazolinones and Microwave-Assisted Synthesis of 3-aryl Quinazolinones in Ethanol." Croatica chemica acta 92, no. 4 (2020): 511–17. http://dx.doi.org/10.5562/cca3597.

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In this study, two fast and efficient protocols for green synthesis of 3-substituted quinazolinones were perfomed. A synthesis of 2-methyl-3-substituted quinazolinones was performed in natural deep eutectic solvents, while 3-aryl quinazolinones were obtained by using microwave assisted synthesis. Benzoxazinone, which was used as an intermediate in the synthesis of 2-methyl-3-substituted quinazolinones, was prepared conventionally from anthranilic acid and acetic anhydride. In order to find the most appropriate synthetic path, twenty natural deep eutectic solvents were applied as a solvent in t

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Tran, Huu Tam, Oanh Nhu Thi Vu, Thuy Nhu Thi Le, Bao Dam Chau Nguyen, and Ngoc Nguyen Vo. "Substitution to Position Number 2 of 4(3H)-Quinazolinone to Create New Derivatives and to Test the Antibacterial or Antifungal Effects." Applied Sciences 12, no. 5 (2022): 2710. http://dx.doi.org/10.3390/app12052710.

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The campaign “No action today, no cure tomorrow” against antimicrobial resistance proposed by the World Health Organization (WHO) has not only propeled people to take action to prevent antimicrobial resistance, but has also encouraged researchers to develop new antimicrobial agents. 4(3H)-quinazolinone and its derivatives belong to a group of compounds with many potential applications; this study was conducted to find new derivatives of heterocyclic 4(3H)-quinazolinone with biological effects, contributing to research on antibacterial and antifungal compounds. Using the closed-loop method betw

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Kumar, Pratyoosh, Nausheen Amber, and Vishwa Deepak Tripathi. "A Catalyst Free Surfactant Mediated Multicomponent Synthesis of Quinazolinone Derivatives in Aqueous Media." European Journal of Advanced Chemistry Research 4, no. 3 (2023): 1–9. http://dx.doi.org/10.24018/ejchem.2023.4.3.139.

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A versatile and green synthetic protocol has been developed for synthesis of substituted quinazolinone and spiroquinazolinone heterocycles effectively via a combined surfactant mediated system. The use of Surfactant, water as reaction medium, room temperature, high yield and ease of purification made the process very effective and ecofriendly in nature. To demonstrate the wide scope of reaction Isatoic anhydride and Isatin used as reactants in different sets of reactions that leads to formation of Quinazolinones and spiroquinazolinones. A total of 12 derivatives has been prepared and character

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Yang, Fan, Wei-Ping He, Jia-Qi Yao, Dong Zou, Pu Chen, and Jie Li. "Synthesis and Neuroprotective Biological Evaluation of Quinazolinone Derivatives via Scaffold Hopping." Current Organic Synthesis 16, no. 5 (2019): 772–75. http://dx.doi.org/10.2174/1570179416666190328233501.

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Objective: To develop efficient method for the synthesis of quinazolinone derivatives bearing different functional groups on ring A and ring B and evaluation as neuroprotective agents. Methods: Synthetic route to quinazolinone derivatives was furnished by condensation/cyclocondensation/ reduction sequence of the activated N-acylbenzotriazoles. The structures of the targets compounds have been deduced upon their spectral data (1HNMR, 13CNMR and Mass spectroscopy). The neuroprotective activities of the synthesized compounds are also evaluated. Results: Preliminary screening on a MPP+ induced SH-

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Shafii, Behnaz, Mina Saeedi, Mohammad Mahdavi, Alireza Foroumadi, and Abbas Shafiee. "Novel Four-Step Synthesis of Thioxo-quinazolino[3,4-a]quinazolinone Derivatives." Synthetic Communications 44, no. 2 (2013): 215–21. http://dx.doi.org/10.1080/00397911.2013.800211.

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Huang, Cheng, Yuan Fu, Hua Fu, Yuyang Jiang, and Yufen Zhao. "Highly efficient copper-catalyzed cascade synthesis of quinazoline and quinazolinone derivatives." Chemical Communications, no. 47 (2008): 6333. http://dx.doi.org/10.1039/b814011a.

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Starikova, A. A., A. A. Tsibizova, N. V. Zolotareva, D. V. Merezhkina, A. A. Ozerov, and M. A. Samotrueva. "New derivatives of quinazolinone as an object in the search for substances that exhibit a multi-target effect." Сибирский научный медицинский журнал 44, no. 1 (2024): 155–71. http://dx.doi.org/10.18699/ssmj20240116.

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Due to the rapid growth in the number of patients with diabetes in a complicated epidemiological picture, the question of the possibility of exposure of a substance to several targets becomes more important. It is noted that the most common infectious diseases in patients with diabetes mellitus are infections of the respiratory and urinary tract, skin and soft tissues, diabetic foot ulcers, otitis media and periodontal infections. Antimicrobial agents can have both direct and indirect hypoglycemic effects. Quinazolinones belonging to the group of heterocyclic derivatives exhibit a wide range o

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