Recent insight into BACE1 as a potential target for treatment of Alzheimer's disease

Atta, Asmaa M.; Darwish, Khaled M.; Elgawish, Mohamed Saleh; Moustafa, Samia Mahmoud; Helal, Mohamed A.

doi:10.21608/rpbs.2021.55758.1087

Cited by 2 publications

(1 citation statement)

References 49 publications

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“…Therefore, inhibiting acetylcholine degradation by cholinesterase enzymes can be a promising tactic for treatment of AD. Currently, there are just four acetylcholinesterase inhibitors approved by FDA for AD treatment: tacrine (withdrawn because of hepatotoxicity), rivastigmine, donepezil and galantamine (Figure 1) (Atta, darwish et al 2021) (Marucci, Buccioni et al 2021). It's worth mentioning that the aim of our present study is to design and synthesis novel compounds act as acetylcholinesterase inhibitors and used for treatment of AD.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Molecular docking Investigations of Ring-Fused Benzimidazoles as Novel Acetylcholinsterase Inhibitors

Ghareb

Atta

Elrayess

2023

Records of Pharmaceutical and Biomedical Sciences

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Alzheimer's disease (AD) is a highly neurodegenerative brain disease and is the most prevalent type of dementia. AD affects parts of brain that are responsible for memory, language and thought. Cholinergic hypothesis proposed that deficiency of acetylcholine in certain zones of brain may be responsible for the progressive memory deterioration observed in patient with AD. Therefore, inhibition of acetylcholinesterase (AChE) may represent a hopeful target for treatment of AD. Herein, new series of ring-fused benzimidazoles (benzimidazo [1,2-c] quinazoline derivatives (scheme 1, compounds 2a-d) and benzimidazo [2,1-c] triazole derivatives (scheme 2, compounds 7 and 8a-b) as main scaffolds) were synthesized using benzene1,2-diamine as a starting material and characterized by mass spectroscopy, IR, 1 HNMR, 13 C NMR and elemental analysis. Molecular docking studies were performed on AChE and demonstrated the preferential binding interaction of synthesized compounds with AChE binding site. Therefore, the obtained results imply that ring-fused benzimidazoles may act as an auspicious lead compounds for further optimization and biological evaluation against AChE.

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Section: Introductionmentioning

confidence: 99%