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Evaluation of Anti-Inflammatory and Anti-Tubercular Activity of 4-Methyl-7-Substituted Coumarin Hybrids and Their Structure Activity Relationships

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Заглавие Evaluation of Anti-Inflammatory and Anti-Tubercular Activity of 4-Methyl-7-Substituted Coumarin Hybrids and Their Structure Activity Relationships
 
Автор Nibin, Joy, M.
Guda, M. R.
Zyryanov, G. V.
 
Тематика ANTI-INFLAMMATORY ACTIVITY
ANTI-TUBERCULAR ACTIVITY
COUMARINS
SAR
4 METHYL 7 HYDROXY COUMARIN
COUMARIN DERIVATIVE
DICLOFENAC
ISONIAZID
ISONIAZID PLUS RIFAMPICIN
N,N DIMETHYLFORMAMIDE
PYRIDONE DERIVATIVE
RESAZURIN
RIFAMPICIN
TUBERCULOSTATIC AGENT
UNCLASSIFIED DRUG
ANTIINFLAMMATORY ACTIVITY
ARTICLE
DENATURATION
HUMAN
IN VITRO STUDY
MICROWAVE IRRADIATION
MINIMUM INHIBITORY CONCENTRATION
MYCOBACTERIUM FORTUITUM
MYCOBACTERIUM SMEGMATIS
MYCOBACTERIUM TUBERCULOSIS
STRUCTURE ACTIVITY RELATION
SUBSTITUTION REACTION
 
Описание Four sets of previously synthesized 4-methyl-7-substituted coumarin derivatives were screened for their in vitro anti-inflammatory and anti-tubercular activities. The anti-inflammatory potential of 3a–t, 5a–o, 6a–n, and 7a–f synthesized compounds was evaluated by an anti-denaturation assay using diclofenac sodium as the reference standard. Evaluation of the anti-tuberculous activity of the mentioned compounds was performed by the Resazurin test method against four different TB strains using rifampicin and isoniazid as reference drugs. Based on the anti-inflammatory results, compounds 3o, 5f, 6c, and 7d proved to be the most active compounds in their respective series. Additionally, compounds 3k–n, 5b–d, 6d–f, 6k, 7a, and 7f were found to be the most potent anti-tuberculous agents. In fact, most of the screened compounds exhibited promising activity profiles compared to the respective standard drugs. The structure–activity connections revealed a few intriguing aspects, indicating that the presence of electron-donating and nitrogen-rich fragments boost the anti-inflammatory effects of the examined compounds. However, the presence of electron-withdrawing substituents was required to boost the anti-tubercular activity of the evaluated compounds. © 2023 by the authors.
Ministry of Education and Science of the Russian Federation, Minobrnauka; Ural Federal University, UrFU; Ministry of Science and Higher Education of the Russian Federation
All the authors are grateful to the Russian Federation’s Ministry of Science and Higher Education and Ural Federal University, Russia, for support.
This research was funded by the Ministry of Science and Higher Education of the Russian Federation, (Ural Federal University Program of Development within the Priority-2030).
 
Дата 2024-04-05T16:33:08Z
2024-04-05T16:33:08Z
2023
 
Тип Article
Journal article (info:eu-repo/semantics/article)
|info:eu-repo/semantics/publishedVersion
 
Идентификатор Nibin Joy, M, Guda, M & Zyryanov, G 2023, 'Evaluation of Anti-Inflammatory and Anti-Tubercular Activity of 4-Methyl-7-Substituted Coumarin Hybrids and Their Structure Activity Relationships', Pharmaceuticals, Том. 16, № 9, 1326. https://doi.org/10.3390/ph16091326
Nibin Joy, M., Guda, M., & Zyryanov, G. (2023). Evaluation of Anti-Inflammatory and Anti-Tubercular Activity of 4-Methyl-7-Substituted Coumarin Hybrids and Their Structure Activity Relationships. Pharmaceuticals, 16(9), [1326]. https://doi.org/10.3390/ph16091326
1424-8247
Final
All Open Access, Gold, Green
https://www.scopus.com/inward/record.uri?eid=2-s2.0-85172442081&doi=10.3390%2fph16091326&partnerID=40&md5=face08c51f2e41d3a6a903aae4b0788c
https://www.mdpi.com/1424-8247/16/9/1326/pdf?version=1695135598
http://elar.urfu.ru/handle/10995/130805
10.3390/ph16091326
85172442081
001072628200001
 
Язык en
 
Права Open access (info:eu-repo/semantics/openAccess)
cc-by
https://creativecommons.org/licenses/by/4.0/
 
Формат application/pdf
 
Издатель Multidisciplinary Digital Publishing Institute (MDPI)
 
Источник Pharmaceuticals
Pharmaceuticals