Synthesis, molecular docking evaluation for LOX and COX-2 inhibition and determination of in-vivo analgesic potentials of aurone derivatives
In: Heliyon, Jg. 10 (2024), Heft 9, S. e29658-
Online
academicJournal
Zugriff:
In the current study, seven (7) aurone derivatives (ADs) were synthesized and employed to in-vitro LOX and COX-2 assays, in-vivo models of acetic acid-induced mice writhing, formalin-induced mice paw licking and tail immersion test to evaluate their analgesic potential at the doses of 10 mg and 20 mg/kg body weight. Molecular docking was performed to know the active binding site at both LOX and COX-2 as compared to standard drugs. Among the ADs, 2-(3,4-dimethoxybenzylidene)benzofuran-3(2H)-one (WE-4)possessed optimal LOX and COX-2 inhibitory strength (IC50=0.30 μM and 0.22 μM) as compared to standard (ZileutonIC50 = 0.08 μM, CelecoxibIC50 = 0.05 μM). Similarly in various pain models compound WE-4 showed significantly (p
| Titel: |
Synthesis, molecular docking evaluation for LOX and COX-2 inhibition and determination of in-vivo analgesic potentials of aurone derivatives
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| Autor/in / Beteiligte Person: | Ikram, Muhammad ; Shah, Ismail ; Hussain, Haya ; Ehsan Ullah Mughal ; Naeem, Nafeesa ; Sadiq, Amina ; Nazir, Yasir ; Syed Wadood Ali Shah ; Zahoor, Muhammad ; Ullah, Riaz ; Ali, Essam A. ; Muhammad Naveed Umar |
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| Zeitschrift: | Heliyon, Jg. 10 (2024), Heft 9, S. e29658- |
| Veröffentlichung: | Elsevier, 2024 |
| Medientyp: | academicJournal |
| ISSN: | 2405-8440 (print) |
| DOI: | 10.1016/j.heliyon.2024.e29658 |
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