Thieno2,3-bpyridine amines: Synthesis and evaluation of tacrine analogs against biological activities related to Alzheimer's disease

Saeedi, M. and Safavi, M. and Allahabadi, E. and Rastegari, A. and Hariri, R. and Jafari, S. and Bukhari, S.N.A. and Mirfazli, S.S. and Firuzi, O. and Edraki, N. and Mahdavi, M. and Akbarzadeh, T. (2020) Thieno2,3-bpyridine amines: Synthesis and evaluation of tacrine analogs against biological activities related to Alzheimer's disease. Archiv der Pharmazie, 353 (10).

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In search of safer tacrine analogs, various thieno2,3-bpyridine 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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Uncontrolled Keywords: 1,2,3,4,5,8,9,10,11,12 decahydrocycloheptaecyclohepta4,5 thieno2,3 bpyridin 13 amine; 1,2,3,4,7,8,9,10 octahydrobenzo4,5thieno2,3 bquinolin 11 amine; 1,2,3,4,7,8,9,10,11 nonahydrocycloheptaecyclohexa4,5thieno 2,3 bpyridin 12 amine; 1,2,3,6,7,8 hexahydrocyclopentaecyclopenta4,5thieno2,3 bpyridin 9 amine; 1,2,3,6,7,8,9 heptahydrocyclopentaecyclohexa4,5thieno2,3 bpyridin 10 amine; 1,2,3,6,7,8,9,10 octahydrocycloheptaecyclopenta4,5thieno2,3 bpyridin 11 amine; 1,2,3,6,7,8,9,10 octahydrocyclopentaecyclohepta4,5thieno2,3 bpyridin 11 amine; 2 benzyl 1,2,3,4,6,7,8,9 octahydropyrido4',3':4,5thieno2,3 bquinolin 5 amine; 2 benzyl 1,2,3,4,6,7,8,9,10 nonahydrocycloheptaepyrido 4',3':4,5thieno2,3 bpyridin 5 amine; 2,3,4,7,8,9,10,11 octahydro 1h cyclohepta4,5thieno2,3 bquinolin 12 amine; 2,3,6,7,8,9 hexahydro 1h cyclopenta4,5thieno2,3 bquinolin 10 amine; amyloid protein; cholinesterase inhibitor; donepezil; neuroprotective agent; pyridine derivative; tacrine; tacrine derivative; thieno2,3 bpyridine amine derivative; unclassified drug, Alzheimer disease; Article; cell damage; cholinesterase inhibition; controlled study; drug screening; drug synthesis; enzymatic assay; Hep-G2 cell line; human; IC50; lipophilicity; melting point; molecular docking; neuroprotection; priority journal; proton nuclear magnetic resonance; selectivity index; stereospecificity
Subjects: WL Nervous System
Depositing User: eprints admin
Date Deposited: 16 Jun 2021 04:19
Last Modified: 16 Jun 2021 04:19

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