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Academic literature on the topic 'Quinazoline-4(3H)-ones'

Author: Grafiati
Published: 18 May 2024

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Journal articles on the topic "Quinazoline-4(3H)-ones"

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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 (November 1, 2021): 163–70. http://dx.doi.org/10.31603/pharmacy.v7i2.4827.

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The 3-(benzylideneamino)-2-(2,4-dichlorophenyl)-quinazoline-4(3H)-ones (BDCQ) are compounds developed as anticancer drugs and quinazolines. The activity and bioavailability of BDCQ derivatives as anticancer compounds that inhibit COX-2 can be predicted by computer programs and online servers. Substituents are added at positions 2 and 3 to the quinazoline-4(3H)-on ring, such as -H, -NO2, -OCH3, -N(CH3)2, -SO2NH2, -OH, and –OCH3. QSAR as COX-2 inhibitor analysis was performed by SPSS Ver. 21 software. Lipinski’s rule of five for determining bioavailability is performed by an online server at http://ilab.acdlabs.com. The best QSAR equation used to predict the COX-2 inhibitors from these compounds is RS-pred = 0.372 Log P + 0.014 MR + 0.979 Etot – 4.859, with n= 12, R = 0.998; SE = 0.356, F = 805.252 and sig = 0.001. Six compounds were predicted to have good oral bioavailability, such as 3-(benzylideneamino)-2-(2,4-dichlorophenyl)quinazoline-4(3H)-one, 2-(2,4-dichlorophenyl)-3-((2-nitrobenzylidene)amino)quinazoline-4(3H)-one, 2-(2,4-dichlorophenyl)-3-((3-nitrobenzylidene)amino)quinazoline-4(3H)-one, 2-(2,4-dichlorophenyl)-3-((2-methoxybenzilidene)amino)quinazoline-4(3H)-one, 2-(2,4-dichlorophenyl)-3-((3-methoxybenzylidene)amino)quinazolin-4(3H)-one, and 2-(((2-(2,4-dichlorophenyl)-4-oxoquinazolin-3(4H)-yl)imino)methyl)- benzenesulfonamide. This research can be used as an in vitro and in vivo study for BDCQ derivatives as anticancer drugs.
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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-phenylquinazolin-3(4H)-ylamino)quinazolin-4(3H)-one (9h) emerged as the most active compounds of the series. These compounds have shown most potent antibacterial activity against the tested organisms ofProteus vulgarisandBacillus subtilishaving zone of inhibition values of 1.1 cm and 1.4 cm for compound9a1.2 cm and 1.0 cm for compound9h, respectively.
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Špirková, Katarína, and Štefan Stankovský. "Annelation to the Quinazoline Ring. Preparation of Some Substituted 2H-Imidazo- and 2,3-Dihydropyrimido[1,2-c]quinazolines." Collection of Czechoslovak Chemical Communications 61, no. 6 (1996): 957–61. http://dx.doi.org/10.1135/cccc19960957.

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Preparation of some substituted 2H-imidazo[1,2-c]quinazolin-3-ones (2a-2f) and 2,3-dihydropyrimido[1,2-c]quinazolin-4-ones (3a-3c) by reaction of corresponding 3H-quinazoline-4-thiones (1a-1d) with amino acid esters is described. IR, 1H NMR and 13C NMR spectra of the compounds synthesized are presented.
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Tiwari, Abhishek R., and Bhalchandra M. Bhanage. "Transition-metal free synthesis of quinazolinones via tandem cyclization of 2-halobenzoic acids with amidines." RSC Advances 5, no. 70 (2015): 57235–39. http://dx.doi.org/10.1039/c5ra11159e.

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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 (April 30, 2021): 077–84. http://dx.doi.org/10.30574/ijbpsa.2021.1.2.0027.

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Background: Quinazoline and quinazolinone scaffolds represent an important class of biologically active nitrogen heterocyclic compounds. Many marketed drugs are based on these moieties. A diverse range of molecules with quinazoline/quinazolinone moieties have been reported to exhibit broad spectrum of biological activities Objective: This study is aimed at the synthesis of these quinazolinone derivatives, quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one and evaluate them for their antibacterial activities. Method: The consolidation of 2-amino-methyl-4-methoxybenzoate with acetic anhydride produced the cyclic compound 2-methyl-4, 5-disubstituted-1, 3-benzo-oxazine-4-one which also produce a novel 2,3-disubstituted quinazolin-4 ones via the reaction with hydrazine hydrate. The quinazolinone derivatives quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one were evaluated pharmacologically for their in vivo analgesic activities by acetic acid induced writhing in mice. The compounds synthesized were assuredly validated by means of Infrared, Nuclear Magnetic Resonance (1H and 13C), Gas Chromatography Mass Spectrophotometer and Elemental analysis. The synthesized compounds were tested for their antibacterial activity.Compounds 1,2 and 3 showed significant antibacterial activities. Discussion: Compound 1 was identified by the absence of methyl group and the presence of methyl group for compound 2. The test analysed compounds exhibited significant antibacterial activities. The compounds synthesized exhibited promising antibacterial activities against the tested organisms. Conclusion: The compounds have high antibacterial activities. Compound 2 has a higher activity compared to Compound 1 and 3. Compound 2 has a higher antibacterial against Escherichia coli, Klebsiella pneumonia and Pseudomonas aeuriginosa
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Oluwaseye, Adedirin, A. UZAIRU, G. A. SHALLANGWA, and S. E. ABECHI. "QSAR STUDIES ON DERIVATIVES OF QUINAZOLINE-4(3H)-ONES WITH ANTICONVULSANT ACTIVITIES." Journal of Engineering and Exact Sciences 4, no. 2 (July 4, 2018): 0255–64. http://dx.doi.org/10.18540/jcecvl4iss2pp0255-0264.

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Srivastav, Manish, MD Salahuddin, and S. M. Shantakumar. "Synthesis and Anti-inflammatory Activity of Some Novel 3-(6-Substituted-1, 3-benzothiazole-2-yl)-2-[{(4-substituted phenyl) amino} methyl] quinazolines-4 (3H)-ones." E-Journal of Chemistry 6, no. 4 (2009): 1055–62. http://dx.doi.org/10.1155/2009/507052.

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A series of novel 3-(6-substituted-1, 3-benzothiazole-2-yl)-2-[{(4-substituted phenyl) amino} methyl] quinazolines-4(3H)-ones were synthesized by treating 2-(chloromethyl)-3-(6-substituted-1, 3-benzothiazole-2-yl) quinazoline-4-(3H)-one (IIa-d) with various substituted amine. The compounds (IIa-d) prepared by treating 2-[(chloroacetyl) amino] benzoic acid with different 2-amino-6-substituted benzothiazole. Elemental analysis, IR,1HNMR and mass spectral data confirmed the structure of the newly synthesized compounds. Synthesized quinazolines-4-one derivative were investigated for their anti-inflammatory and antibacterial activity.
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Wright, William B., Andrew S. Tomcufcik, Peter S. Chan, Joseph W. Marsico, and Jeffery B. Press. "Thromboxane synthetase inhibitors and antihypertensive agents. 4. N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-ones." Journal of Medicinal Chemistry 30, no. 12 (December 1987): 2277–83. http://dx.doi.org/10.1021/jm00395a016.

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Barlaam, Bernard, Craig S. Harris, Jonathan Lecoq, and Ha Thi Hoang Nguyen. "Preparation of 6-aminoquinazolin-4(3H)-ones via direct SNAr on the quinazoline ring." Tetrahedron 68, no. 2 (January 2012): 534–43. http://dx.doi.org/10.1016/j.tet.2011.11.008.

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Naidu, P. Paradesi, Akula Raghunadh, K. Raghavendra Rao, Ramamohan Mekala, J. Moses Babu, B. R. Rao, V. Siddaiah, and Manojit Pal. "Urea/Thiourea as Ammonia Surrogate: A Catalyst-Free Synthesis of 2-Substituted 2,3-Dihydroquinazolin-4(1H)-ones/Quinazoline-4(3H)-ones." Synthetic Communications 44, no. 10 (April 29, 2014): 1475–82. http://dx.doi.org/10.1080/00397911.2013.862551.

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Dissertations / Theses on the topic "Quinazoline-4(3H)-ones"

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Tiwari, Bipransh Kumar. "Studies on antiproliferative and antibacterial properties of some quinazoline-4(3H)-ones and their dimers." Thesis, University of North Bengal, 2016. http://ir.nbu.ac.in/hdl.handle.net/123456789/2573.

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