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Information × Registration Number 0221U104749, 0118U004370 , R & D reports Title Purposeful search of anti-inflammatory agents among condensed and spiro-condensed quinazoline derivatives popup.stage_title Head Kovalenko Sergiy I, Доктор фармацевтичних наук Registration Date 07-04-2021 Organization Zaporizhzhya State Medical University popup.description2 Similar chinazolines and their condensed analogues have always attracted the attention of scientists as objects of promising research aimed at the development of new medicinal products. This fact is explained by the high biologic activity as natural, and synthetic chinazolines and, without a doubt, their broad possibilities of chemical modification. These approaches led to the discovery and creation of a whole group of "leader spoluks", especially with markedly antiparasitic action. In the course of scientific research by the methods of molecular docking the possible mechanisms of realization of antiphlogistic action of substituted, condensed and spiro-condensed chinazolines were found for the first time, promising directions of construction of potent antiphlogistics in the mentioned reactions were determined. High antiphlogistic activity of (3H-quinazolin-4-ylidene)hydrazide products of N-degraded amino acids and products of their cyclization was determined. We developed and implemented the strategy of the search of antiflammatory agents among 3'-R1-spiro[(aza/oxa/tia)heterocyclyl-1(3,4),6'-[1,2,4]triazino[2,3-c]quinazolin]-2'(7'H)-ones. It has been found that the interaction of 2-(1H-tetrazol-5-yl)anylin, 2-(3-R-1H-1,2,4-triazol-5-yl)anylin, 6-R-3-(2-aminophenyl)-1,2, 4-triazin-5-ones with γ-ketocarboxylic acids and their natural products is used to obtain unidentified intermediates with pyrrolo[1, 2-a]tetrazolo[1,5-c]quinazolinic, pyrolo[1,2-a][1,2,4]triazino[2,3-c]quinazolinic, pyrolo[1,2-a][1,2,4]triazolo[1,5-c]quinazolinic fragments. The peculiarities of formation of 6,6-disamined 6,7-dihydro-2H-[1,2,4]triazino[2,3-c]quinazolin-2-one based on the reaction of 6-R-3-(2-aminophenyl)-1,2,4-triazin-5-one with ketocarboxylic acids were found. Product Description popup.authors Antypenko Olena M Bukhtyiarova Nina V Voskoboinik Oleksii Yu Kinichenko Hanna O Kovalenko Serhii I Korzhova Alla S Krasovska Nataliia I Miedviedieva Kateryna P Maletska Olena R Martynenko Yulia V Moskalenko Oleksandra S Nahorna Nataliia O Nosulenko Inna S Stavytskyi Viktor V Kholodniak Olena V Kholodnyak Sergii V Shabelnyk Kostyantyn P popup.nrat_date 2021-04-07 Close