DSpace About DSpace Software
 

IRZSMU >
Кафедри >
Кафедра фармацевтичної, органічної та біоорганічної хімії >
Наукові праці. (Фармацевтична хімія) >

Please use this identifier to cite or link to this item: http://dspace.zsmu.edu.ua/handle/123456789/21645

Название: [1,2,4]triazino[2,3-c] quinazoline hybrids with azole and azine heterocycles: design, synthesis, antibacterial and antiradical activity
Авторы: Grytsak, O. A.
Schabelnyk, K. P.
Kinichenko, A.
Komarovska-Porokhnyvets, O.
Lubеnets, V.
Voskoboinik, O.
Kovalenko, S.
Грицак, О. А.
Шабельник, Костянтин Петрович
Кініченко, Анна Олександрівна
Ключевые слова: heterocyclic hybrids
synthesis
radical scavenging activity
antimicrobial and antifungal activity
SAR-analysis
Issue Date: 2024
Библиографическое описание: [1,2,4]triazino[2,3-c] quinazoline hybrids with azole and azine heterocycles: design, synthesis, antibacterial and antiradical activity / O. Grytsak, K. Schabelnyk, A. Kinichenko, O. Komarovska-Porokhnyvets, V. Lubеnets, O. Voskoboinik, S. Kovalenko // ScienceRise: Pharmaceutical Science. - 2024. - N 6. - P. 4-14. - https://doi.org/10.15587/2519-4852.2024.318160.
Аннотация: The aim. Present paper devoted to the purposeful search of a promising biologically active compounds among heterocyclic hybrids combining in their structure [1,2,4]triazino[2,3-c]quinazoline system and a “pharmacophoric” azole or azine fragment, joined through an alkylthio linker group. Material and methods. Methods of synthetic organic chemistry were used to prepare target compounds. The purity and structure of the synthesized compounds were confirmed by elemental analysis, HPLC-MS, and ¹H NMR spectrometry. Radical-scavenging activity was estimated using DPPH-assay, antimicrobial activity was studied by serial dilution method. Results. A combinatorial library of 30 novel heterocyclic hybrids was designed and synthesized. The target compounds were obtained via the interaction of 6-chloroalkyl-3-R-2H-[1,2,4]triazino[2,3-c]quinazolin-2-ones and corresponding heterocyclic thiones in the presence of a base. The synthesized compounds were studied for their radical scavenging and antimicrobial activity. Most of the obtained compounds revealed low antimicrobial activity against studied strains. However, the heterocyclic hybrid combining triazinoquinazoline, thiadiazole, and 4-fluorophenyl moieties (compound 2.14) inhibited the growth of S. aureus, E. coli, and M. luteum. Among the obtained compounds, five heterocyclic hybrids demonstrated significant DPPH radical scavenging activity (30.41–43.53 %). The “structure-activity” correlations were evaluated and discussed. It was estimated that “linker” alkylthio-group modification resulted in the most pronounced changes in the radical scavenging activity of obtained compounds. Conclusions. Triazinoquinazoline-based heterocyclic hybrids are promising objects for further screening for antimicrobial activity and pharmacological effects associated with antiradical properties.
URI: http://dspace.zsmu.edu.ua/handle/123456789/21645
Appears in Collections:Студентське наукове товариство: статті, доповіді, тези
Наукові праці. (Фармакогнозія)
Наукові праці. (Фармацевтична хімія)

Files in This Item:

File Description SizeFormat
318160-Article Text-741203-1-10-20241231.pdf1,55 MBAdobe PDFView/Open
View Statistics

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

 

Valid XHTML 1.0! DSpace Software Copyright © 2002-2010  Duraspace - Feedback