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Journal articles on the topic 'Quinazolin-4(3H)-one; antibacterial activity; Nucleophile'

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Published: 4 June 2025

Last updated: 1 August 2025

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1

Osarumwense, Osarodion Peter. "Synthesis and antibacterial activity of 3-amino-6-iodo-2-methyl quinazolin 4-(3H)-one and 6-iodo-2-methyl-4H-benzo [D] [1, 3] oxazin-4-one." World Journal of Advanced Research and Reviews 2, no. 3 (2019): 014–20. https://doi.org/10.5281/zenodo.4309464.

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Quinazolines and its derivatives represent one of the most active classes of compounds, which possess wide range of biological activities like anti-bacterial, analgesic, anti-microbial, anti-inflammatory, anticancer, and anti-hypertensive ,antifungal, anti-HIV, antioxidant, analgesic, anticonvulsant, antimalarial, antitumor, anti-tubercular activities. The objective of the present study was to synthesize these quinazolinone derivatives 6-iodo-2-methyl-4H-benzo[d]-[1,3]-oxazin-4-one and 3-amino-6-iodo-2—methyl-3H-quinazolin-4-one and evaluate them for their antibacterial activity. 6-lodo-

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2

Osarumwense, Peter Osarodion. "Synthesis and antibacterial 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." GSC Biological and Pharmaceutical Sciences 11, no. 1 (2020): 212–20. https://doi.org/10.5281/zenodo.4277223.

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The current study is aimed at the synthesis of these quinazolinone derivatives 7-Chloro-2-Methyl-4H-benzo[d]-[1,3]-Oxazin-4-one and 3-Amino-7-Chloro-2—Methyl-3H-Quinazolin-4-One and evaluate them for their antibacterial activity.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 7-chloro-2-methyl-4H-benzo[d][1,3]-oxazin-4-one and 3-amino-7-chloro-2-me

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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-

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4

Appani, Ramgopal, Baburao Bhukya, and Kiran Gangarapu. "Synthesis and Antibacterial Activity of 3-(Substituted)-2-(4-oxo-2-phenylquinazolin-3(4H)-ylamino)quinazolin-4(3H)-one." Scientifica 2016 (2016): 1–5. http://dx.doi.org/10.1155/2016/1249201.

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A series of novel 3-(substituted)-2-(substituted quinazolinylamino)quinazolin-4(3H)-ones were synthesized by the reaction of 3-(substituted)-2-hydrazino-quinazoline-4(3H)-ones with 2-phenyl-3,1-benzoxazin-4-one. The starting materials 3-(substituted)-2-hydrazino-quinazolin-4(3H)-ones were synthesized from various primary amines by a multistep synthesis. All the title compounds were tested for their antibacterial activity using ciprofloxacin as reference standard. Compounds 3-(4-fluorophenyl)-2-(4-oxo-2-phenylquinazolin-3(4H)-ylamino)quinazolin-4(3H)-one (9a) and 3-(4-chlorophenyl)-2-(4-oxo-2-p

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5

Sulthana, M. T., K. Chitra, and V. Alagarsamy. "Anti-HIV, Antitubercular and Antibacterial Activities of Novel 3-(Substituted Quinazolinylamino)-2-phenyl quinazolin-4(3H)ones." Asian Journal of Chemistry 32, no. 2 (2019): 281–86. http://dx.doi.org/10.14233/ajchem.2020.22280.

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In the present study, we have synthesized a series of novel 2-phenyl-3-(substituted quinazolinylamino)quinazolin-4(3H)-ones by the reaction of 3-(substituted)-2-hydrazinoquinazoline-4(3H)-ones with 2-phenyl-3,1-benzoxazin-4-one. The starting material 3-(substituted)-2-hydrazinoquinazolin-4(3H)-ones were synthesized from various primary amines. All the synthesized compounds were screened for their antitubercular, anti-HIV and antibacterial activity against different Grampositive and Gram-negative strains by agar dilution method. Among the test compounds, 3-(4-nitrophenyl)-2-(4-oxo-2-phenylquina

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Azab, M. E., E. A. Kassab, M. A. El-Hashash, and R. S. Ali. "Synthesis and Antibacterial Activity of Some New 4(3H)Quinazolin-4-one Derivatives." Phosphorus, Sulfur, and Silicon and the Related Elements 184, no. 3 (2009): 610–25. http://dx.doi.org/10.1080/10426500802243182.

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7

Khan, Ayad Kareem. "Facile Synthesis, Characterization of New Quinazolinones with Different Azo Compounds, 1,2,3-Triazole Moieties and Evaluation Their Anti-bacterial Activity." Al-Mustansiriyah Journal of Science 28, no. 3 (2018): 122. http://dx.doi.org/10.23851/mjs.v28i3.180.

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In the present research, a series of some azo compounds (5-9) and 1,2,3-triazoles derived from 2-methyl quinazolin-4(3H)-one were synthesized successfully by stepwise routes includes the following: 3-amino-2-methylquinazolin-4(3H)-one (3) prepared firstly by conversion of 2-aminobenzoic acid into methyl 2-aminobenzoate (1) followed by reaction with acetic anhydride to form methyl -2-acetamidobenzoate (2). The amide then allowed reacting with hydrazine hydrate to give compound (3). Diazotization reaction with sodium nitrite in the presence of hydrochloric acid yield the 3-(chlorodiazenyl)-2-met

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8

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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9

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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Charanjeet, Singh, Yaswant, and Sharma Mukesh. "SYNTHESIS AND ASSESSMENT THE IN-VITRO ANTIOXIDANT ACTIVITY OF 2,3-DISUBTITUTED QUINAZOLIN-4(3H)-ONE DERIVATIVES." International Journal of Current Pharmaceutical Review and Research 12, no. 2 (2020): 01–11. https://doi.org/10.5281/zenodo.12667459.

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Quinazolinones have various biological activities such as anticancer, antibacterial,antidiabetic, anticonvulsant, antihistaminic, antiinflammatory, antifungal, anthelmintics andantiviral activities. In this research some of compounds 2,3-disubtituted quinazolin-4(3H)-one derivatives had been synthesized under microwave irradiation. The compounds wereobtained from reaction some of benzoxazine derivatives with hydrazine hydrate usingmicrowave irradiation and the result of reaction we obtained 82-96%. The products had beentested by IR, 1H-NMR, 13C-NMR and Mass Spectroscopy analysis. The using mic

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11

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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Eweas, Ahmad Farouk, Qasem Mahmoud Aref Abdallah, and Mohamed Fouad Elbadawy. "Synthesis and biological evaluation of some new 2-pyridylquinazoline derivatives." Current Chemistry Letters 10, no. 4 (2021): 459–70. http://dx.doi.org/10.5267/j.ccl.2021.4.005.

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2-pyridyl [3H]-quinazolin-4-one derivatives fused or substituted with different oxygen or nitrogen heterocycle moieties as potential anti-tumor and anti-microbial agents were prepared, characterized and biologically screened. The synthesis process started from 5-bromo-2-[pyridin-4-ylcarbonyl]amino]benzoic acid which was converted to the crucial building block 6-Bromo-2-(pyridin-4-yl)quinazolin-4(3H)-one via two alternative routes. Compound 3 underwent halogenation reaction POCl3 and PCl5 to afford compound 6-Bromo-4-chloro-2-(pyridin-4-yl)quinazoline 4. The novel cyclized products 5a,b-10 were

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13

Osarumwense Peter Osarodion. "Design, synthesis and antibacterial activity of novel metal complex of 3-amino-2-methyl 6-1odo quinazolin-4(3H)-one." International Journal of Frontiers in Biology and Pharmacy Research 3, no. 1 (2022): 001–8. http://dx.doi.org/10.53294/ijfbpr.2022.3.1.0044.

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Introduction: 4(3H)-quinazolinone rings have been reported to possess different biological activities such as antibacterial, antifungal, antitubercular, antiviral, anticancer. These activities also include antihypertensive, diuretic, antimicrobial, pesticidal, anticonvulsant, anaesthetic and sedative activities, anti-malarial, and anti-diabetic.The above observations and findings stimulated my interest to synthesize these novel, Co (ll) , Cu (ll) and Zn (ll) complexes of 3-amino-2-methyl-6-lodo-quinazolin-4 (3H)-one compounds. Methods: A new Ligand 3-amino-2-methyl 6-Iodo quinazolin-4(3H)-One

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14

Wang, Xiang, Juan Yin, Li Shi, Guoping Zhang, and Baoan Song. "Design, synthesis, and antibacterial activity of novel Schiff base derivatives of quinazolin-4(3H)-one." European Journal of Medicinal Chemistry 77 (April 2014): 65–74. http://dx.doi.org/10.1016/j.ejmech.2014.02.053.

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15

Mendogralo, Elena Y., Larisa Y. Nesterova, Ekaterina R. Nasibullina, et al. "The Synthesis and Biological Evaluation of 2-(1H-Indol-3-yl)quinazolin-4(3H)-One Derivatives." Molecules 28, no. 14 (2023): 5348. http://dx.doi.org/10.3390/molecules28145348.

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The treatment of many bacterial diseases remains a significant problem due to the increasing antibiotic resistance of their infectious agents. Among others, this is related to Staphylococcus aureus, especially methicillin-resistant S. aureus (MRSA) and Mycobacterium tuberculosis. In the present article, we report on antibacterial compounds with activity against both S. aureus and MRSA. A straightforward approach to 2-(1H-indol-3-yl)quinazolin-4(3H)-one and their analogues was developed. Their structural and functional relationships were also considered. The antimicrobial activity of the synthe

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16

Peter Osarodion, Osarumwense. "Synthesis and Analgesic Activity of 3-(3-methoxyphenyl)-2-methylsulfanyl-3Hquinazolin-4-one (4) and 3-(3-methoxyphenyl)-2-thioxo-2,3-dihydro1H-quinazolin-4-one (3) Via N-(3- methoxyphenyl)-methyl dithiocarbamic acid (2)." Endocrine System and Diabetes 2, no. 1 (2023): 01–05. http://dx.doi.org/10.58489/2836-502x/007.

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Introduction: 4(3H)-quinazolinone rings have been reported to possess different biological activities such as antibacterial, antifungal, antitubercular, antiviral, anticancer. These activities also include antihypertensive, diuretic, antimicrobial, pesticidal, anticonvulsant, anaesthetic and sedative activities, anti-malarial, and anti-diabetic. Methods/Experimental: The compound, 3-(3-methoxyphenyl)-2-thioxo-2,3-dihydro1H-quinazolin-4-one (3) was synthesized by dissolving Methyl anthranilate and N-(3- methoxyphenyl)-methyl dithiocarbamic acid in ethanol and anhydrous potassium carbonate and r

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17

Öztürk, S., S. Okay, and A. Yıldırım. "Synthesis, anticorrosion, antibacterial, and antifungal activity of new amphiphilic compounds possessing quinazolin-4(3H)-one scaffold." Russian Chemical Bulletin 69, no. 11 (2020): 2205–14. http://dx.doi.org/10.1007/s11172-020-3023-0.

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18

Salih, Nadia Adil. "SYNTHESIS OF SOME NEW QUINAZOLIN-4(3H)-ONE DERIVATIVES AND STUDY OF THEIR SOME ANTIBACTERIAL ACTIVITY." Journal of Al-Nahrain University Science 11, no. 2 (2008): 16–23. http://dx.doi.org/10.22401/jnus.11.2.03.

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19

Ramadan, Sayed K., and Eman A. E. El-Helw. "Synthesis and Antimicrobial Activity Evaluation of Some Novel Heterocycles Derived from Chromonyl-2(3H)-furanone." Journal of Chemical Research 42, no. 6 (2018): 332–36. http://dx.doi.org/10.3184/174751918x15295796734379.

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6-Chloro-3-((2-oxo-5-phenylfuran-3(2 H)-ylidene)methyl)-4 H-chromen-4-one was utilised for the construction of N-heterocycles. The proclivity of this furanone towards some nitrogen nucleophiles, i.e. glycine, thiosemicarbazide, thiocarbohydrazide, phenylhydrazine and o-phenylenediamine, was studied. The structures of all products obtained were established on the basis of their analytical and spectral data. All synthesised compounds were screened for their in vitro antibacterial (two strains of bacteria; Escherichia coli and Staphylococcus aureus) and antifungal (two fungus strains; Aspergillus

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Zhu, Mei, Yan Li, Xuesha Long, Congyu Wang, Guiping Ouyang, and Zhenchao Wang. "Antibacterial Activity of Allicin-Inspired Disulfide Derivatives against Xanthomonas axonopodis pv. citri." International Journal of Molecular Sciences 23, no. 19 (2022): 11947. http://dx.doi.org/10.3390/ijms231911947.

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Xanthomonas axonopodis pv. citri (Xac) belongs to the Gram-negative species, causing citrus canker that seriously affects the fruit yield and quality of many rutaceae plants. Herein, we found that compound 2-(butyldisulfanyl) quinazolin-4(3H)-one exhibited remarkable anti-Xac activity in vitro with a half effective concentration (EC50) of 2.6 μg/mL, while the positive controls thiodiazole-copper with 57 μg/mL and bismerthiazol with 68 μg/mL and this compound showed great anti-citrus canker activity in vivo. This active compound also was confirmed to reduce biofilm formation, increase the level

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Patel, Navin B., Jaymin C. Patel, and Gaman G. Barat. "In vitro evaluation of the antibacterial and antifungal activity of some new pyrazolyl-quinazolin-4(3H)-one derivatives." Medicinal Chemistry Research 21, no. 2 (2010): 229–38. http://dx.doi.org/10.1007/s00044-010-9530-z.

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Sulthana M.T, Chitra K, and Alagarsamy V. "Synthesis of novel 4-oxo-N-(4-oxo-3-substituted-3,4-dihydroquinazolin-2-yl amino)-2-phenylquinazoline-3(4H)-carboxamidines as AntiHIV, antitubercular and antibacterial agents." International Journal of Research in Pharmaceutical Sciences 10, no. 3 (2019): 2186–92. http://dx.doi.org/10.26452/ijrps.v10i3.1449.

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A series of novel 4-oxo-N-(4-oxo-3-substituted-3,4-dihydroquinazolin-2-yl amino)-2-phenylquinazoline-3(4H)-carboxamidines are prepared from methyl 4-oxo-2-phenylquinazoline-3(4H)-carbthioimidate & 3-(substituted)-2-hydrazino-quinazoline-4(3H)-ones. The starting material 4-oxo-2-phenylquinazoline-3(4H)-carbthioimidates were prepared from anthranilic acid while the 3-(substituted)-2-hydrazino-quinazolin-4(3H)-one was prepared from a range of 1° amines using multistep preparation. Entire synthesized analogues were screened for their antitubercular, anti-HIV and antibacterial activity. Among t

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Samotrueva, M. A., A. A. Ozerov, A. A. Starikova, et al. "ANTIMICROBIAL ACTIVITY STUDY OF NEW QUINAZOLIN-4(3H)-ONES AGAINST STAPHYLOCOCCUS AUREUS AND STREPTOCOCCUS PNEUMONIAE." Pharmacy & Pharmacology 9, no. 4 (2021): 318–29. http://dx.doi.org/10.19163/2307-9266-2021-9-4-318-329.

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Quinazolin-4(3H)-one derivatives exhibiting a wide spectrum of a pharmacological activity, represent a promising class of substances used to obtain antibacterial agents, which is especially important in the context of the emergence of pathogenic microorganisms’ resistance to drugs used in medicine. It has been proved that compounds having a naphthyl radical in the molecule, as well as an amide group bound to the benzene ring as quinazolinone substituents, are characterized by a pronounced antimicrobial activity against Staphylococcus aureus and Streptococcus pneumoniae.The aim of the research

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N., B. Patel, and N. Patel J. "Synthesis and biological activity of some new 1,3-thiazolyl-6-bromoquinazolin-4(3H)ones." Journal of Indian Chemical Society Vol. 86, Nov 2009 (2009): 1231–36. https://doi.org/10.5281/zenodo.5823662.

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Department of Chemistry, Veer Narmad South Gujarat University, Surat-395 007, Gujarat, India <em>E-mail </em>: drnavin@satyam.net.in <em>Manuscript received 15 December 2008, revised 11 June 2009, accepted 3 July 2009</em> The title compound 1,3-thiazolyl-6-bromoquinazolin-4(3<em>H</em>)ones 5<sub>t-xv</sub> have been synthesized from the molecule 2-[(2,6-dichlorophenyl)amino]phenyl acetic acid 1 through multi-step reaction sequence. The structures of new compounds have been confirmed by elemental analyses, IR, <sup>1</sup>H and <sup>13</sup>C NMR spectral data. All the compounds wer

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Gaman, Barat* Navin Patel. "SYNTHESIS AND IN VITRO PHARMACOLOGICAL STUDIES OF SOME NOVEL PRECURSORS OF 6, 8-DIBROMOQUINAZOLIN-4(3H) ONE." INTERNATIONAL JOURNAL OF ENGINEERING SCIENCES & RESEARCH TECHNOLOGY 5, no. 12 (2016): 465–72. https://doi.org/10.5281/zenodo.203855.

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A novel series of some precursors of 6, 8-dibromoquinazolin-4(3H)-one 61-12 have been synthesized by the based catalysed cyclisation of chromenamido 51-12 with phenylhydrazine hydrate. The overall reaction was base catalysed conventional multistep process. The title compounds have been confirmed by spectral data IR, 1H NMR, 13C NMR and elemental analysis. All the synthesized target molecules were screened for gram positive, gram negative antibacterial and fungicidal activity In Vitro by disc diffusion method. The zone of inhibition measured and calculated potency. The pharmacological strength

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Osarumwense, P. O. "Synthesis and Analgesic Activity of 3-Amino-6-Bromo-2-Methyl Quinazolin-4(3H) –One and 6-Bromo-2-Methyl-4H-Benzo[D] [1,3]- Oxazin-4-One." Continental J. Applied Sciences 12, no. 3 (2017): 29–39. https://doi.org/10.5281/zenodo.995719.

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<em>The current study is aimed at the synthesis and Analgesic evaluation of quinazolinone derivatives. The condensation of Methyl-2-amino-5-bromobenzoate with acetic anhydride yielded the cyclic compound 2-methyl 6-bromo-1, 3-benzo-oxazine-4-one which further produce 3-Amino-2-Methyl 6-bromoquinazolin4(3H)-ones via the reaction with hydrazine hydrate. The compounds synthesized were unequivocally confirmed by means of Chromatography Mass Spectrophotometer and Elemental analysis. The quinazolonones were evaluated pharmacologically for their in-vivo analgesic activities by acetic acid induced wri

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Hmidet, A. B. S., A. L. Yasenyavskaya, A. A. Tsibizova, I. N. Tyurenkov, A. A. Ozerov, and M. A. Samotrueva. "Evaluation of the antimicrobial activity of pyrimidine compound 3-(2-benzyloxy-2-oxoethyl)quinazoline-4(3H)-oh in relation to Klebsiella pneumoniae." Antibiotics and Chemotherapy 68, no. 1-2 (2023): 22–26. http://dx.doi.org/10.37489/0235-2990-2023-68-1-2-22-26.

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The study is devoted to the evaluation of the antimicrobial activity against Klebsiella pneumoniae of the pyrimidine compound 3-(2-Benzyloxy-2-oxoethyl)quinazoline-4(3H)-one under in vivo conditions in a model of generalized infection. The experiment was performed on 40 CBA line mice, which were divided into four groups: Group 1, control animals that received intraperitoneal injection water in an equivalent volume (control I); Group 2, infected animals that received no treatment (control II); Group 3, mice with generalized infection that received ceftriaxone at a dose of 50 mg/kg intraperitone

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Osarumwense, Peter, and Osaro Iyekowa. "Synthesis and Antibacterial Activity of 7-chloro-2–methyl-4H-benzo[d][1,3]–oxazin-4-one and 3–amino-7-chloro-2-methyl quinazolin-4(3H)–one." Tropical Journal of Natural Product Research 1, no. 4 (2017): 173–75. http://dx.doi.org/10.26538/tjnpr/v1i4.7.

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Osarumwense, Osarodion Peter. "Synthesis and antibacterial activity of 3-amino-6-iodo-2-methyl quinazolin 4-(3H)-one and 6-iodo-2-methyl-4H-benzo [D] [1, 3] oxazin-4-one." World Journal of Advanced Research and Reviews 2, no. 3 (2019): 014–20. http://dx.doi.org/10.30574/wjarr.2019.2.3.0041.

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Osarumwense Peter Osarodion. "Synthesis and antibacterial 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." GSC Biological and Pharmaceutical Sciences 11, no. 1 (2020): 212–20. http://dx.doi.org/10.30574/gscbps.2020.11.1.0110.

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Natesan, Gopal, Appalaraju Velaga, Nelycia Su Yean Tze, and Soon An Nie. "Antibacterial activity of newer Quinazolin-4(3H)-one derivatives." Frontiers in Pharmacology 9 (2018). http://dx.doi.org/10.3389/conf.fphar.2018.63.00101.

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El-Subbagh, Hussein I., and Mohamed A. Sabry. "2-Substituted-mercapto-quinazolin-4(3H)-ones as DHFR inhibitors." Mini-Reviews in Medicinal Chemistry 21 (March 4, 2021). http://dx.doi.org/10.2174/1389557521666210304105736.

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: Antifolates are a class of drugs used as antibacterial, antiparasitic, and anticancer agents. This review focuses on 2-substituted-mercapto-quinazolin-4(3H)-one analogues as dihydrofolate reductase (DHFR) inhibitors. Several research efforts have concluded a structural model for this class of 2-thio-quinazoline derivatives to get compounds with remarkable biological activity. The pattern and orientation of the -system substitutions with regard to the quinazoline nucleus manipulate the activity. The application of the obtained model criteria produced compounds 18, 20, and 21, which proved to

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Osarodion, Osarumwense Peter. "Synthesis And Antibacterial Activity of 6-Bromo-2-(O-Aminophenyl)-3-Amino-Quinazolin-4(3h)-One From 6-Bromo,2-(O-Aminophenyl)-3,1-Benzoxazin-4(3h)-One." Clinical Case Reports and Trails 2, no. 3 (2023). http://dx.doi.org/10.58489/2836-2217/014.

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Introduction: Quinazolinone derivatives reveal various medicinal properties such as analgesic, anti-inflammatory and anticancer activities, as well as antimicrobial activity. These heterocycles are valuable intermediates in organic synthesis.Methods/Experimental: The compound, 6-bromo,2-(o-aminophenyl)-3,1-benzoxazin-4(3H)-one (1) was synthesized by dissolving 5-bromo anthranillic acid in 100 ml of pyridine. To this reaction mixture o-amino benzoyl chloride stirring at room temperature for 30 minutes this was refluxed with 75 mL of hydrazine hydrate for 3 hrs at 120-1300C. the reaction mixture

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Маркосян, А. И., А. C. Айвазян, С. А. Габриелян, М. Ю. Дангян та А. Г. Аракелян. "Синтез и антибактериальная активность производных 3-аллил-5,5-диметил-2-тиоксо-2,3,5,6-тетрагидробензо[h]хиназолин-4(1H)-она". Chemical Journal of Armenia, 9 листопада 2023, 228–38. http://dx.doi.org/10.54503/0515-9628-2023.76.3-228.

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Alkylation of 3-allyl-5,5-dimethyl-2-thioxo-2,3,5,6-tetrahyd-robenzo[h]quinazo-line-4(1H)-one (thioxobenzoquinazoline) was alkylated in an alkaline medium with halides of various structures, resulting in the formation of 2-sulfanylsubstituted 3-allyl-5,5-dimethyl-5,6-dihydrobenzo[h]quinazolin-4(3H)-ones. The condensation of thioxobenzohquinazoline with hydrazine hydrate yielded 3-allyl-2-hydrazinyl-5,5-dimethyl-5,6-dihydroben-zo[h]quinazoline-4(3H)-one. However, analogous reactions with 2-ethanolamine and 3-propanolamine proceeded anomalously, resulting in the formation of 2-(2-hydroxyethyl)am

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"Design, Synthesis and Antibacterial Activity of Novel Metal Complex of 3-Amino-2-Methyl 6-1odo Quinazolin-4(3H)-one." Journal of Clinical & Experimental Immunology 7, no. 3 (2022). http://dx.doi.org/10.33140/jcei.07.03.02.

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Introduction: 4(3H)-quinazolinone rings have been reported to possess different biological activities such as antibacterial, antifungal, antitubercular, antiviral, anticancer. These activities also include antihypertensive, diuretic, antimicrobial, pesticidal, anticonvulsant, anaesthetic and sedative activities, anti-malarial, and anti-diabetic. The above observations and findings stimulated my interest to synthesize these novel, Co (ll), Cu (ll) and Zn (ll) complexes of 3-amino-2-methyl-6-lodo-quinazolin-4 (3H)-one compounds. Methods/Experimental: A new Ligand 3-amino-2-methyl 6-Iodo quinazol

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Muthu Boopathi, Gopal, and Shanmugarajan T. S. "Synthesis, Characterisation and Antimicrobial Activity of Novel 2-Methyl-3-(2-(substituted ylidene)hydrazinyl)quinazolin-4(3H)-ones." Research Journal of Pharmacy and Technology, May 30, 2022, 2176–83. http://dx.doi.org/10.52711/0974-360x.2022.00362.

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Several novel quinazolinones were designed and synthesized from anthranilic acid by a multistep synthesis. Structures of synthesized compounds were well characterized using FT-IR, 1H-NMR, Mass spectroscopy and bases of elemental analysis. Entire test compounds were screened for their antibacterial and antifungal activities by agar streak dilution test against various pathogenic strains of bacteria and fungi. Antimicrobial studies revealed that all title compounds exhibited mild to good antibacterial activity and mild to moderate antifungal activity. The relationship between the functional grou

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Samotrueva, M., A. Starikova, N. Zolotareva та ін. "COMPUTER SIMULATION OF THE PROCESSES COMPLEXATION BETWEEN NEW DERIVATIVES OF QUINAZOLINE-4(3H)-ONE, QUINAZOLINE-2,4(1H,3H)-DIONE AND CYTOCHROME P-450 STEROL-7Α-HYDROXYLASE(CYP27A1) WHEN STUDYING THEIR ANTIMICROBIAL EFFECTS AGAINST KLEB.PNEUMONIAE". Problems of Biological, Medical and Pharmaceutical Chemistry, 14 травня 2025, 3–11. https://doi.org/10.29296/25877313-2025-04-01.

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Introduction. Multi-resistance of Klebsiella pneumoniae to known antimicrobial agents determines the need for urgent development of new drugs ex-hibiting an antibacterial effect. Compounds used in the treatment of non-infectious pathologies, affecting various protein targets and realizing the "anti-microbial potential", seem promising in the search for new derivatives. Of particular interest is the predicted high probability of inhibition of sterol-27-hydroxylase cytochrome P-450 (CYP27A1) by new derivatives of quinazoline-4(3H)-one and quinazoline-2,4(1H,3H)-dione with the possibility of prev

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Aditya, Sahu. "New Derivatives of (E)-3-(5-((substitutedphenylamino)methyl)-1,3,4-thiadiazol-2-yl)-2-styryl quinazolin-4(3H)-one: Searching for New Antifungal and Antibacterial Agents." February 4, 2021. https://doi.org/10.5281/zenodo.4500441.

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Objective: The objective of the paper was to evaluate the antifungal and antibacterial potential of new derivatives of ((E)-3-(5-((substitutedphenylamino)methyl)-1,3,4-thiadiazol-2-yl)-2-styryl quinazolin-4(3H)-one. Materials and Methods: Various syntheses of (E)-3-(5-(substitutedaminomethyl)-1,3,4-thiadiazol-2-yl)-2-styrylquinazolin-4(3H)-one derivatives have been synthesized by reacting 2-substituted benzoxazin-4-one with (E)-2-(4-Substituedstyryl)-4H-benzo[d] [1,3]oxazin-4-one. All synthesized compounds have been characterized by the infrared, 1HNMR, and mass spectral analysis. Proposed com

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"Synthesis and Antibacterial Activity of 6-bromo-2-(o-aminophenyl)-3-amino-Quinazolin-4(3H)-one from 6-bromo,2-(o-aminophenyl)-3,1-benzoxazin-4(3H)-one." Advances in Image and Video Processing 11, no. 3 (2023). http://dx.doi.org/10.14738/aivp.113.14235.

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Verma, Priyanka, Lai Zhen Xiang, Udit Chaube, and Gopal Natesan. "Synthesis, Antimicrobial Evaluation, Molecular Docking and Dynamics Simulations of Novel 2,3‐Disubstituted Quinazolin‐4(3H)‐one Derivatives." ChemistrySelect 9, no. 36 (2024). http://dx.doi.org/10.1002/slct.202403009.

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AbstractThe rise of multidrug‐resistant organisms (MDROs) represents a significant challenge to healthcare, underscoring the need for novel antimicrobial agents. Quinazolinone compounds, noted for their diverse biological activities, particularly at the 2nd and 3rd positions, in conjunction with sulphanilamide and isatin derivatives, present a promising avenue for antibacterial development. This study focuses on the synthesis of novel 2,3‐disubstituted quinazolin‐4(3H)‐one derivatives from Schiff base intermediates GA3A and GA3B. The synthesis involved the reaction of 2‐(substituted phenyl)‐4H

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Peter Osarodion, Osarumwense. "Synthesis and Antibacterial Activity of 2-[o-imino-(4-thiazolidinone)-phenyl]-3-imino-(4-thiazolidinone)- 6-bromo Quinazolin-4(3H)-one from 2-(o-thiadiaminephenyl)-3-thiadiamine-6-bromo–quinazoline-4(3H)-one." American Journal of Materials Synthesis and Processing, May 10, 2023. http://dx.doi.org/10.11648/j.ajmsp.20230801.11.

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Patel, Jeevan Lal, Naveen Kumar Sureddy, Raju Chedupaka, Venkatesham Papisetti, S. P. Mahapatra, and Santhosh Penta. "New Quinazolinone‐Tethered 1,2,3‐Triazoles aSs Potent Antimicrobial Agents: Design, Synthesis, Biological Evaluation and in silico Docking Study." ChemistrySelect 9, no. 30 (2024). http://dx.doi.org/10.1002/slct.202400876.

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AbstractNovel 1,2,3‐triazole acetamide linked quinazolinone derivatives were synthesized via click reaction, by reacting of 3‐methyl‐2‐(prop‐2‐yn‐1‐ylthio)quinazolin‐4(3H)‐one with various aryl azides as prominent fungal pathogen Candida albicans interactions. The prepared triazole compounds were characterized using mass spectrometry, 1H NMR, 13C NMR, and IR spectroscopic techniques. Compounds were screened for their in vitro antibacterial and antifungal activity against a variety of microorganisms namely, Bacillus subtilis, Enterococcus faecalis, Klebsiella pneumonia, Escherichia coli, Asperg

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Norouzi, Fateme Haji, Naser Foroughifar, Alireza Khajeh-Amiri, and Hoda Pasdar. "A novel powerful Choline Chloride – Thiourea /Sulfuric Acid, efficient and recyclable catalyst via microwave‐assisted for the synthesis of Quinazolin- 4(3H)–one derivatives as Antibacterial Agents in green media." Current Microwave Chemistry 09 (March 24, 2022). http://dx.doi.org/10.2174/2213335609666220324145341.

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Background: Choline Chloride - Thiourea / Sulfuric Acid is a powerful and efficient green catalyst used for one-pot synthesis of quinazoline-4 (3H) -one derivatives via a reaction between various amines, acetic anhydride, and anthranilic acid under microwave irradiation and solvent-free conditions (4a-q). Microwave irradiation, which is a faster, more cost-effective, less energy-intensive, and more efficient method than conventional heating, has been used to synthesize some quinazolinone derivatives. Introduction: For the past ten years, one of the major subjects in synthetic organic chemistry

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Sulthana, M. T., V. Alagarsamy, and K. Chitra. "Design, Synthesis, Pharmacological evaluation, in silico modeling, prediction of toxicity and metabolism studies of novel 1-(substituted)-2-methyl-3-(4-oxo-2-phenyl quinazolin-3(4H)-yl)isothioureas." Medicinal Chemistry 16 (August 17, 2020). http://dx.doi.org/10.2174/1573406416666200817153033.

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Background: Although exhaustive efforts to prevent and treat tuberculosis (TB) was taken the problem still continues due to multi-drug-resistant (MDR) and extensively drug resistant TB (XDR-TB). It clearly highlights the urgent need to develop novel “druggable” molecules for the co-infection treatment and strains of MDR-TB and XDR-TB. Objective: In this approach a hybrid molecule was created by merging two or more pharmacophores. Active site of targets may be addressed by each of the pharmacophores and proffers the opportunity for selectivity. In addition, it also reduced the undesirable side

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