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Please use this identifier to cite or link to this item: http://dspace.zsmu.edu.ua/handle/123456789/15389

Название: Substituted 3-R-2,8-Dioxo-7,8-dihydro-2H-pyrrolo[1,2-a][1,2,4] triazino [2,3-c]quinazoline-5a(6H)carboxylic Acids and their Salts-a Promising Class of Anti-inflammatory Agents
Авторы: Stavytskyi, V. V.
Antypenko, O. M.
Nosulenko, I. S.
Berest, G. G.
Voskoboinik, O. Yu.
Kovalenko, S. I.
Ставицький, Віктор Валерійович
Антипенко, Олексій Миколайович
Носуленко, Інна Степанівна
Берест, Галина Григорівна
Воскобойнік, Олексій Юрійович
Коваленко, Сергій Іванович
Ключевые слова: anti-inflammatory activity
drug design
3-(2-aminophenyl)-6-R-1,2,4-triazin-5(2H)ones
pyrrolo[1,2-a][1,2,4]triazino[2,3-c]quinazolines
molecular docking
SAR
Issue Date: 2021
Издатель: Sharjah : Bentham Science Publishers
Библиографическое описание: Substituted 3-R-2,8-Dioxo-7,8-dihydro-2H-pyrrolo[1,2-a][1,2,4] triazino [2,3-c]quinazoline-5a(6H)carboxylic Acids and their Salts-a Promising Class of Anti-inflammatory Agents / V. V. Stavytskyi, O. M. Antypenko, I. S. Nosulenko, G. G. Berest, O. Yu. Voskoboinik, S. I. Kovalenko // Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry. - 2021. – Vol. 20, №1. - P. 75-88. - https://doi.org/ 10.2174/1871523019666200505073232
Аннотация: Abstract: Background: Fragment-based drug design as well as in silico pre-screening of affinity to biological targets are among the most effective methods of medicinal chemistry. Abovementioned approaches were used for purposeful search of anti-inflammatory agents among quinazoline condensed derivatives. Objective: Purposeful synthesis of novel 3-R-2,8-dioxo-7,8-dihydro-2H-pyrrolo[1,2-a][1,2,4]triazino[2,3-c]quinazoline-5a(6H)carboxylic acids and their salts as promising anti-inflammatory agents, evaluation of their structure by physicochemical methods and establishing of their anti-inflammatory activity. Method: The structures of target compounds were proposed due to principles of fragment-based drug design. The features of the synthesized compounds structures were evaluated by IR-, NMR spectroscopy and chromatography-mass spectrometry and were discussed in detail. Probable molecular mechanisms of activity were predicted due to molecular docking. The anti-inflammatory activity was determined by their ability to reduce the formalin- and carrageenan-induced paw edema in rats.
URI: http://dspace.zsmu.edu.ua/handle/123456789/15389
Appears in Collections:Наукові праці. (Клінічна фармація ФПО)
Наукові праці. (Фармакогнозія)
Наукові праці. (Органічна хімія)

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