دورية أكاديمية
Evaluation of Anti-Inflammatory and Anti-Tubercular Activity of 4-Methyl-7-Substituted Coumarin Hybrids and Their Structure Activity Relationships
| العنوان: | Evaluation of Anti-Inflammatory and Anti-Tubercular Activity of 4-Methyl-7-Substituted Coumarin Hybrids and Their Structure Activity Relationships |
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| المؤلفون: | Nibin, Joy, M., Guda, M. R., Zyryanov, G. V. |
| المصدر: | Pharmaceuticals |
| بيانات النشر: | Multidisciplinary Digital Publishing Institute (MDPI) |
| سنة النشر: | 2023 |
| المجموعة: | Ural Federal University (URFU): ELAR / Уральский федеральный университет: электронный архив УрФУ |
| مصطلحات موضوعية: | 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 |
| الوصف: | 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). |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | application/pdf |
| اللغة: | English |
| تدمد: | 1424-8247 |
| العلاقة: | 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/ph16091326Test; 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/ph16091326Test; 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=face08c51f2e41d3a6a903aae4b0788cTest; https://www.mdpi.com/1424-8247/16/9/1326/pdf?version=1695135598Test; http://elar.urfu.ru/handle/10995/130805Test; 85172442081; 001072628200001 |
| DOI: | 10.3390/ph16091326 |
| الإتاحة: | https://doi.org/10.3390/ph16091326Test http://elar.urfu.ru/handle/10995/130805Test https://www.mdpi.com/1424-8247/16/9/1326/pdf?version=1695135598Test |
| حقوق: | info:eu-repo/semantics/openAccess ; cc-by ; https://creativecommons.org/licenses/by/4.0Test/ |
| رقم الانضمام: | edsbas.D3BFDD11 |
| قاعدة البيانات: | BASE |
Full Text Finder | تدمد: | 14248247 |
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| DOI: | 10.3390/ph16091326 |