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

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

Saeedi M^{1, 2} ; Safavi M³ ; Allahabadi E⁴ ; Rastegari A² ; Hariri R⁴ ; Jafari S³ ; Bukhari SNA⁵ ; Mirfazli SS⁶ ; Firuzi O⁷ ; Edraki N⁷ ; Mahdavi M⁸ ; Akbarzadeh T^{2, 4}

Show Affiliations

1. Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
2. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran
3. Department of Biotechnology, Iranian Research Organization for Science and Technology (IROST), Tehran, Iran
4. Department of Medicinal Chemistry, Faculty of Pharmacy, 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

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

Style	Citing Format
MLA	Saeedi M, et al.. "Thieno[2,3-B]Pyridine Amines: Synthesis and Evaluation of Tacrine Analogs Against Biological Activities Related to Alzheimer's Disease." Archiv der Pharmazie, vol. 353, no. 10, 2020, pp. -.
APA	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. Archiv der Pharmazie, 353(10), -.
Chicago	Saeedi M, Safavi M, Allahabadi E, Rastegari A, Hariri R, Jafari S, Bukhari SNA, et al.. "Thieno[2,3-B]Pyridine Amines: Synthesis and Evaluation of Tacrine Analogs Against Biological Activities Related to Alzheimer's Disease." Archiv der Pharmazie 353, no. 10 (2020): -.
Harvard	Saeedi M et al. (2020) 'Thieno[2,3-B]Pyridine Amines: Synthesis and Evaluation of Tacrine Analogs Against Biological Activities Related to Alzheimer's Disease', Archiv der Pharmazie, 353(10), pp. -.
Vancouver	Saeedi M, Safavi M, Allahabadi E, Rastegari A, Hariri R, Jafari S, et al.. Thieno[2,3-B]Pyridine Amines: Synthesis and Evaluation of Tacrine Analogs Against Biological Activities Related to Alzheimer's Disease. Archiv der Pharmazie. 2020;353(10):-.
BibTex	@article{ author = {Saeedi M and Safavi M and Allahabadi E and Rastegari A and Hariri R and Jafari S and Bukhari SNA and Mirfazli SS and Firuzi O and Edraki N and Mahdavi M and Akbarzadeh T}, title = {Thieno[2,3-B]Pyridine Amines: Synthesis and Evaluation of Tacrine Analogs Against Biological Activities Related to Alzheimer's Disease}, journal = {Archiv der Pharmazie}, volume = {353}, number = {10}, pages = {-}, year = {2020} }
RIS	TY - JOUR AU - Saeedi M AU - Safavi M AU - Allahabadi E AU - Rastegari A AU - Hariri R AU - Jafari S AU - Bukhari SNA AU - Mirfazli SS AU - Firuzi O AU - Edraki N AU - Mahdavi M AU - Akbarzadeh T TI - Thieno[2,3-B]Pyridine Amines: Synthesis and Evaluation of Tacrine Analogs Against Biological Activities Related to Alzheimer's Disease JO - Archiv der Pharmazie VL - 353 IS - 10 SP - EP - PY - 2020 ER -

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Abstract