Purposeful search and characteristic of anti-inflammatory activity of sodium (3-R-2-оxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)alkylcarboxylates and their halogen containing analogues
Aim. The approaches for creating novel agents with anti-inflammatory activity among sodium (3-R-2-oxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)alkylcarboxylates and their halogen containing analogues were described in presented article. Methods and results. Mentioned methods have been based on c...
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| Format: | Article |
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Zaporizhzhia State Medical and Pharmaceutical University
2016-04-01
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| Series: | Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki |
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| Online Access: | http://pharmed.zsmu.edu.ua/article/view/62036/58068 |
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| author | V. V. Yakubovska N. М. Seredinska О. Yu. Voskoboynik G. І. Stepanyuk S. І. Kovalenko |
| author_facet | V. V. Yakubovska N. М. Seredinska О. Yu. Voskoboynik G. І. Stepanyuk S. І. Kovalenko |
| author_sort | V. V. Yakubovska |
| collection | DOAJ |
| description | Aim. The approaches for creating novel agents with anti-inflammatory activity among sodium (3-R-2-oxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)alkylcarboxylates and their halogen containing analogues were described in presented article.
Methods and results. Mentioned methods have been based on combination of «in silico» screening with experimental studies. Affinity of studied compounds to the active center of COX-1 and COX-2 enzymes has been shown. Conducted visualization of compound – active site complex allowed to suppose the presence of anti-inflammatory activity of studied compounds.
Conclusions. It was established, that sodium (3-R-2-oxo-2Н-[1,2,4]triazino[2,3-c]quinazoline-6-yl)alkylcarboxylates and their halogen-containing analogues reveal anti-inflammatory activity, the most active was compound DSK-38 (ED50 – 4 mg/kg as against 8 mg/kg of diclofenac sodium). «Structure–activity» relationships features among studied compounds have been discussed. |
| format | Article |
| id | doaj-art-c73e9ab87fbb42e1923e729d257b8eb9 |
| institution | Kabale University |
| issn | 2306-8094 2409-2932 |
| language | English |
| publishDate | 2016-04-01 |
| publisher | Zaporizhzhia State Medical and Pharmaceutical University |
| record_format | Article |
| series | Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki |
| spelling | doaj-art-c73e9ab87fbb42e1923e729d257b8eb92025-08-20T03:57:47ZengZaporizhzhia State Medical and Pharmaceutical UniversityAktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki2306-80942409-29322016-04-011606610.14739/2409-2932.2016.1.62036Purposeful search and characteristic of anti-inflammatory activity of sodium (3-R-2-оxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)alkylcarboxylates and their halogen containing analoguesV. V. YakubovskaN. М. SeredinskaО. Yu. VoskoboynikG. І. StepanyukS. І. KovalenkoAim. The approaches for creating novel agents with anti-inflammatory activity among sodium (3-R-2-oxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)alkylcarboxylates and their halogen containing analogues were described in presented article. Methods and results. Mentioned methods have been based on combination of «in silico» screening with experimental studies. Affinity of studied compounds to the active center of COX-1 and COX-2 enzymes has been shown. Conducted visualization of compound – active site complex allowed to suppose the presence of anti-inflammatory activity of studied compounds. Conclusions. It was established, that sodium (3-R-2-oxo-2Н-[1,2,4]triazino[2,3-c]quinazoline-6-yl)alkylcarboxylates and their halogen-containing analogues reveal anti-inflammatory activity, the most active was compound DSK-38 (ED50 – 4 mg/kg as against 8 mg/kg of diclofenac sodium). «Structure–activity» relationships features among studied compounds have been discussed.http://pharmed.zsmu.edu.ua/article/view/62036/58068sodium (3-R-2-oxo-2Н-[1 2 4]triazino[2 3-c]quinazolin-6-il)carboxylateshalogen-containing analoguesmolecular dockinganti-inflammatory activity |
| spellingShingle | V. V. Yakubovska N. М. Seredinska О. Yu. Voskoboynik G. І. Stepanyuk S. І. Kovalenko Purposeful search and characteristic of anti-inflammatory activity of sodium (3-R-2-оxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)alkylcarboxylates and their halogen containing analogues Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki sodium (3-R-2-oxo-2Н-[1 2 4]triazino[2 3-c]quinazolin-6-il)carboxylates halogen-containing analogues molecular docking anti-inflammatory activity |
| title | Purposeful search and characteristic of anti-inflammatory activity of sodium (3-R-2-оxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)alkylcarboxylates and their halogen containing analogues |
| title_full | Purposeful search and characteristic of anti-inflammatory activity of sodium (3-R-2-оxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)alkylcarboxylates and their halogen containing analogues |
| title_fullStr | Purposeful search and characteristic of anti-inflammatory activity of sodium (3-R-2-оxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)alkylcarboxylates and their halogen containing analogues |
| title_full_unstemmed | Purposeful search and characteristic of anti-inflammatory activity of sodium (3-R-2-оxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)alkylcarboxylates and their halogen containing analogues |
| title_short | Purposeful search and characteristic of anti-inflammatory activity of sodium (3-R-2-оxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)alkylcarboxylates and their halogen containing analogues |
| title_sort | purposeful search and characteristic of anti inflammatory activity of sodium 3 r 2 оxo 2н 1 2 4 triazino 2 3 c quinazolin 6 yl alkylcarboxylates and their halogen containing analogues |
| topic | sodium (3-R-2-oxo-2Н-[1 2 4]triazino[2 3-c]quinazolin-6-il)carboxylates halogen-containing analogues molecular docking anti-inflammatory activity |
| url | http://pharmed.zsmu.edu.ua/article/view/62036/58068 |
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