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Thieno[2,3-B]Pyridine Amines: Synthesis and Evaluation of Tacrine Analogs Against Biological Activities Related to Alzheimer's Disease Publisher Pubmed



Saeedi M1, 2 ; Safavi M3 ; Allahabadi E4 ; Rastegari A2 ; Hariri R4 ; Jafari S3 ; Bukhari SNA5 ; Mirfazli SS6 ; Firuzi O7 ; Edraki N7 ; Mahdavi M8 ; Akbarzadeh T2, 4
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Source: Archiv der Pharmazie Published:2020


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. © 2020 Deutsche Pharmazeutische Gesellschaft
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