| Title : Thieno[2,3-b]pyridine amines: Synthesis and evaluation of tacrine analogs against biological activities related to Alzheimer's disease - Saeedi_2020_Arch.Pharm.(Weinheim)__e2000101 |
| Author(s) : Saeedi M , Safavi M , Allahabadi E , Rastegari A , Hariri R , Jafari S , Bukhari SNA , Mirfazli SS , Firuzi O , Edraki N , Mahdavi M , Akbarzadeh T |
| Ref : Arch Pharm (Weinheim) , :e2000101 , 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 microM, 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 (betaA) aggregation and beta-secretase 1, neuroprotectivity, and cytotoxicity against HepG2 cells. Our results indicated efficient anti-Alzheimer's activity of the synthesized compounds. |
| PubMedSearch : Saeedi_2020_Arch.Pharm.(Weinheim)__e2000101 |
| PubMedID: 32657467 |
Saeedi M, Safavi M, Allahabadi E, Rastegari A, Hariri R, Jafari S, Bukhari SNA, Mirfazli SS, Firuzi O, Edraki N, Mahdavi M, Akbarzadeh T (2020)
Thieno[2,3-b]pyridine amines: Synthesis and evaluation of tacrine analogs against biological activities related to Alzheimer's disease
Arch Pharm (Weinheim)
:e2000101
Saeedi M, Safavi M, Allahabadi E, Rastegari A, Hariri R, Jafari S, Bukhari SNA, Mirfazli SS, Firuzi O, Edraki N, Mahdavi M, Akbarzadeh T (2020)
Arch Pharm (Weinheim)
:e2000101