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
