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Title: | Synthesis and biological activity evaluation Of 3-[2-(1h-imidazol-2-Yl)alkyl]-2-thioxo-2,3-dihydroquinazolin-4 (1h) -one derivatives |
Authors: | Zavada, Oksana Tkachenko, Olena Kazmirchuk, Volodymyr Zhuravel, Iryna Lebedynets, Vyacheslav Proskurova, Ia. |
Keywords: | 2-(α,β,ω-aminoalkyl)imidazole 2-isothiocyanatobenzoate 3-[2-(1H-imidazol-2-yl)alkyl]-2-thioxo-2,3-dihydroquinazolin-4(1H)-one antibacterial activity antifungal activity |
Issue Date: | Oct-2018 |
Citation: | Synthesis and biological activity evaluation Of 3-[2-(1h-imidazol-2-Yl)alkyl]-2-thioxo-2,3-dihydroquinazolin-4 (1h) -one derivatives / O. O. Zavada, O. V. Tkachenko, V. V. Kazmirchuk, I. O. Zhuravel, V. O. Lebedynets, Ia. O. Proskurova // International Journal of Green Pharmacy. – 2018. – V. 12 (4). – P. 847–854. |
Abstract: | Detection of general patterns of the synthesis of quinazoline derivatives contains a fragment of 2-aminoalkylimidazole and studying their antimicrobial activity. Materials and Methods: Methods of organic synthesis; physical and physicochemical methods of analysis of organic compounds 1Hydrogen nuclear magnetic resonance spectroscopy and elemental analysis were used. Results: To construct a focused library of compounds with potential antimicrobial and antifungal properties, we have chosen a strategy of combining quinazoline fragments with an imidazole residue in one molecule. The possibility of using 2-aminoalkylimidazoles as an amine component in the heterocyclization reaction with o-isothiocyanato esters was considered. 3-Substituted 2-thioxoquinazoline-4-ones were synthesized by the interaction of methyl esters of 4,5-substituted 2-isothiocyanatobenzoic acids with 2-(α,β,ω-aminoalkyl)imidazoles. Experimental study of antimicrobial activity was performed for the obtained substances, which according to the results of virtual screening showed the best results. Conclusions: A virtual library design with structural fragments of quinazoline and imidazole was made. The systematic series of 6,7-substituted 3-[2-(1H-imidazol-2-yl)-alkyl]-2-thioxo-2,3-dihydroquinazolin-4(1H)-one were synthesized. According to the results of the study of the biological effects of the new derivatives of 3-N-(alkylimidazolyl-2) pyrimidine, a number of patterns of connection “chemical structure - antibacterial action” were established and the main directions of the purposeful |
URI: | https://repo.knmu.edu.ua/handle/123456789/22513 |
Appears in Collections: | Наукові праці. Кафедра медичної та біоорганічної хімії |
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