Aminoimidazo[1,2-A]Pyridine Bearing Different Pyrazole Moieties As the Structural Scaffold for the Development of Bace1 Inhibitor; Synthesis, Structural Characterization, in Vitro and in Silico Studies

Aminoimidazo[1,2-A]Pyridine Bearing Different Pyrazole Moieties As the Structural Scaffold for the Development of Bace1 Inhibitor; Synthesis, Structural Characterization, in Vitro and in Silico Studies Publisher Pubmed

Ebrahimi SES¹ ; Iraji A^{2, 3} ; Jelveh K¹ ; Moazzam A⁴ ; Bahadorikhalili S⁵ ; Yahyameymandi A¹ ; Larijani B⁴ ; Biglar M⁴ ; Edraki N³ ; Mahdavi M⁴

Show Affiliations

1. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran
2. Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
3. Central Research laboratory, Shiraz University of Medical Sciences, Shiraz, Iran
4. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
5. Department of Electronic Engineering, Universitat Rovira i Virgili, Tarragona, Spain

Source: Current Organic Synthesis Published:2022

Abstract

Regarding the critical role of amyloid-β plaques in the pathogenesis of Alzheimer's disease, a series of aminoimidazo[1,2-a]pyridine derivatives were designed and synthesized as potential anti-BACE1 agents targeting the production of amyloid-β plaques. In vitro biological results demonstrated that compounds 7b and 7f exhibited the best inhibitory potency against BACE1 with IC50 values of 22.48 ± 2.06 and 30.61 ± 3.48 μM, respectively. Also, the ligandprotein docking evaluations revealed that compounds 7b and 7f could effectively bind with the different pockets of BACE1 through different interactions with the residue of the active site. The results of current studies underline the potential role of aminoimidazo[1,2-a] pyridine-containing pyrazole derivatives for developing novel BACE1 inhibitors. © 2022 Bentham Science Publishers.

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Style	Citing Format
MLA	Ebrahimi SES, et al.. "Aminoimidazo[1,2-A]Pyridine Bearing Different Pyrazole Moieties As the Structural Scaffold for the Development of Bace1 Inhibitor; Synthesis, Structural Characterization, in Vitro and in Silico Studies." Current Organic Synthesis, vol. 19, no. 6, 2022, pp. 685-692.
APA	Ebrahimi SES, Iraji A, Jelveh K, Moazzam A, Bahadorikhalili S, Yahyameymandi A, Larijani B, Biglar M, Edraki N, Mahdavi M (2022). Aminoimidazo[1,2-A]Pyridine Bearing Different Pyrazole Moieties As the Structural Scaffold for the Development of Bace1 Inhibitor; Synthesis, Structural Characterization, in Vitro and in Silico Studies. Current Organic Synthesis, 19(6), 685-692.
Chicago	Ebrahimi SES, Iraji A, Jelveh K, Moazzam A, Bahadorikhalili S, Yahyameymandi A, Larijani B, Biglar M, Edraki N, Mahdavi M. "Aminoimidazo[1,2-A]Pyridine Bearing Different Pyrazole Moieties As the Structural Scaffold for the Development of Bace1 Inhibitor; Synthesis, Structural Characterization, in Vitro and in Silico Studies." Current Organic Synthesis 19, no. 6 (2022): 685-692.
Harvard	Ebrahimi SES et al. (2022) 'Aminoimidazo[1,2-A]Pyridine Bearing Different Pyrazole Moieties As the Structural Scaffold for the Development of Bace1 Inhibitor; Synthesis, Structural Characterization, in Vitro and in Silico Studies', Current Organic Synthesis, 19(6), pp. 685-692.
Vancouver	Ebrahimi SES, Iraji A, Jelveh K, Moazzam A, Bahadorikhalili S, Yahyameymandi A, et al.. Aminoimidazo[1,2-A]Pyridine Bearing Different Pyrazole Moieties As the Structural Scaffold for the Development of Bace1 Inhibitor; Synthesis, Structural Characterization, in Vitro and in Silico Studies. Current Organic Synthesis. 2022;19(6):685-692.
BibTex	@article{ author = {Ebrahimi SES and Iraji A and Jelveh K and Moazzam A and Bahadorikhalili S and Yahyameymandi A and Larijani B and Biglar M and Edraki N and Mahdavi M}, title = {Aminoimidazo[1,2-A]Pyridine Bearing Different Pyrazole Moieties As the Structural Scaffold for the Development of Bace1 Inhibitor; Synthesis, Structural Characterization, in Vitro and in Silico Studies}, journal = {Current Organic Synthesis}, volume = {19}, number = {6}, pages = {685-692}, year = {2022} }
RIS	TY - JOUR AU - Ebrahimi SES AU - Iraji A AU - Jelveh K AU - Moazzam A AU - Bahadorikhalili S AU - Yahyameymandi A AU - Larijani B AU - Biglar M AU - Edraki N AU - Mahdavi M TI - Aminoimidazo[1,2-A]Pyridine Bearing Different Pyrazole Moieties As the Structural Scaffold for the Development of Bace1 Inhibitor; Synthesis, Structural Characterization, in Vitro and in Silico Studies JO - Current Organic Synthesis VL - 19 IS - 6 SP - 685 EP - 692 PY - 2022 ER -

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