| Autor: |
Mohamed S. Othman, Haseena Naz, Fazal Rahim, Hayat Ullah, Rafaqat Hussain, Muhammad Taha, Shoaib Khan, Mohamed A. Fareid, Shimaa M. Aboelnaga, Anas T. Altaleb, Rashid Iqbal, Syed Adnan Ali Shah |
| Jazyk: |
angličtina |
| Rok vydání: |
2024 |
| Předmět: |
|
| Zdroj: |
Results in Chemistry, Vol 10, Iss , Pp 101717- (2024) |
| Druh dokumentu: |
article |
| ISSN: |
2211-7156 |
| DOI: |
10.1016/j.rechem.2024.101717 |
| Popis: |
We have synthesized 1,2,4-triazole bearing benzenesulfonohydrazide analogues (1–21), characterized through different spectroscopic techniques such as 1HNMR, 13CNMR, HREI-MS and were evaluated against Acetylcholinesterase (AChE) and Butyrylcholinesterase (BuChE) enzymes. All the newly synthesized analogues showed excellent to good inhibition potential with IC50 values ranged from 0.30 ± 0.050 to 15.21 ± 0.50 µM (against AChE) and 0.70 ± 0.050 to 18.27 ± 0.60 µM (against BuChE) as compared to the standard drug Donepezil (IC50 = 2.16 ± 0.12 and 4.5 ± 0.11 µM, respectively). Analogues 2 and 4 which were found inactive against these enzymes. However, analogues 17 (IC50 = 0.30 ± 0.050 and 0.70 ± 0.050 µM) and 13 (IC50 = 0.70 ± 0.05 and 1.70 ± 0.050 µM) were found to have potent inhibitory potentials against the targeted enzymes. Structure-activity relationship was carried out which mainly depends upon the nature, position and numbers of the substitution present on phenyl rings that may be electron withdrawing/donating. Molecular docking study was carried out to know about the binding mode of interaction of the most active site of the synthesized analogues with the targeted enzymes. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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