| Affiliation: | 1. Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran;2. Department of Biotechnology, Iranian Research Organization for Science and Technology (IROST), Tehran, Iran;3. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran;4. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran;5. Department of Pharmaceutical Chemistry, College of Pharmacy, Aljouf University, Aljouf, Saudi Arabia;6. Department of Medicinal Chemistry, Iran University of Medical Sciences, Tehran, Iran;7. Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran;8. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran |
| Abstract: | In search of safer tacrine analogs, various thieno[2,3-b]pyridine amine derivatives were synthesized and evaluated for their inhibitory activity against cholinesterases (ChEs). Among the synthesized compounds, compounds 5e and 5d showed the highest activity towards acetylcholinesterase and butyrylcholinesterase, with IC50 values of 1.55 and 0.23 µM, respectively. The most active ChE inhibitors ( 5e and 5d ) were also candidates for further complementary assays, such as kinetic and molecular docking studies as well as studies on inhibitory activity towards amyloid-beta (βA) aggregation and β-secretase 1, neuroprotectivity, and cytotoxicity against HepG2 cells. Our results indicated efficient anti-Alzheimer's activity of the synthesized compounds. |
