- 2-Alkyl(aryl)-quinazolin-4(3 H)-thiones, 2-R-(quinazolin-4(3 H)-ylthio)carboxylic acids and amides: Synthesis, molecular docking, antimicrobial and anticancer properties
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In this study, a series of novel 2-alkyl(aryl)-quinazolin-4(3H)-thiones, 2-R-(quinazolin-4(3H)-ylthio)carboxylic acids and amides were synthesized and evaluated for antimicrobial and anticancer activities. Their structure was confirmed by elemental analys
- Antypenko, Lyudmyla,Kovalenko, Sergiy,Posylkina, Yulia,Nikitin, Vladyslav,Fedyunina, Natalia,Ivchuk, Vitalii
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p. 253 - 265
(2016/02/03)
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- Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors
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The latest scientific findings concerning PDE7 and PDE4 inhibition suggest that selective small-molecule inhibitors of both enzymes could provide a novel approach to treat a variety of immunological diseases. In this context, we describe a new series of quinazoline derivatives from quinazolin-4-thiones which include a substituted biphenyl fragment. Some of these compounds show inhibitory potencies at sub-micromolar levels against the catalytic domain of PDE7.
- Sánchez, Ana I.,Martínez-Barrasa, Valentín,Burgos, Carolina,Vaquero, Juan J.,Alvarez-Builla, Julio,Terricabras, Emma,Segarra, Víctor
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p. 2370 - 2378
(2013/05/09)
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- Synthesis and anticonvulsant activity evaluation of 5-Phenyl-[1,2,4] triazolo[4,3-c]quinazolin-3-amines
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In the present study we describe the syntheses and anticonvulsant activity evaluation of 5-phenyl-[1,2,4]triazolo[4,3-c]quinazolin-3-amine derivatives. Their anticonvulsant activity and neurotoxicity were evaluated by the maximal electroshock seizure test (MES) and the rotarod test, respectively. The majority of the compounds prepared were effective in the MES screens at a dose level of 100 mg/kg. Of these compounds, the most promising was compound 8h, which showed an ED50 value of 27.4 mg/kg and a protective index (PI) value of 5.8. These values were superior to those provided by valproate (ED50 and PI values of 272 and 1.6, respectively) in the MES test in mice. As well as its anti-MES efficacy, the potencies of compound 8h against seizures induced by pentylenetetrazole and thiosemicarbazide were also established, with the results suggesting that the GABAergic system-mediated mechanisms might be involved in its anticonvulsant activity. Copyright
- Zheng, Yan,Bian, Ming,Deng, Xian-Qing,Wang, Shi-Ben,Quan, Zhe-Shan
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p. 119 - 126
(2013/03/29)
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- Synthesis of substituted 2-benzoylaminothiobenzamides and their ring closure to substituted 2-phenylquinazoline-4-thiones
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Acylation of 2-aminothiobenzamide or 2-methylaminothiobenzamide with substituted benzoyl chlorides has been used to synthesise the corresponding 2-benzoyl-aminothiobenzamides whose subsequent sodium methoxide-catalysed ring closure gives the corresponding quinazoline-4-thiones. These compounds were characterised by means of their 1H- and 13C-NMR spectra. The preferred tautomeric form of selected compounds has been discussed on the basis of their 13C-NMR, IR and Raman spectra. It has been found that in the given medium 1-methyl-quinazoline-4-thiones undergo a replacement of the sulphur substituent by oxygen giving 1-methyl-quinazoline-4-ones. In strong acid media, 2-benzoylaminothiobenzamide is cyclised through its sulphur atom to give 2-phenylbenzo[d-1,3]thiazin-4-one.
- Hanusek, Jiri,Hejtmankova, Ludmila,Kubicova, Lenka,Sedlak, Milos
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p. 323 - 337
(2007/10/03)
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