Benzimidazole-Based Schiff Base Hybrid Scaffolds: A Promising Approach to Develop Multi-Target Drugs for Alzheimer’s Disease

A series of benzimidazole-based Schiff base derivatives (1–18) were synthesized and structurally elucidated through 1H NMR, 13C NMR and HREI-MS analysis. Subsequently, these synthetic derivatives were subjected to evaluation for their inhibitory capabilities against acetylcholinesterase (AChE) and b...

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Published in:Pharmaceuticals (Basel, Switzerland) Switzerland), 2023-09, Vol.16 (9), p.1278
Main Authors: Hussain, Rafaqat, Khan, Shoaib, Ullah, Hayat, Ali, Farhan, Khan, Yousaf, Sardar, Asma, Iqbal, Rashid, Ataya, Farid S, El-Sabbagh, Nasser M, Batiha, Gaber El-Saber
Format: Article
Language:English
Subjects:
AChE
Alzheimer's disease
benzimidazole
Benzimidazoles
BuChE and molecular docking
Drug therapy
Drugs
Enzymes
Proteins
SAR
Schiff base
Schiff bases
synthesis
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Summary:A series of benzimidazole-based Schiff base derivatives (1–18) were synthesized and structurally elucidated through 1H NMR, 13C NMR and HREI-MS analysis. Subsequently, these synthetic derivatives were subjected to evaluation for their inhibitory capabilities against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). All these derivatives showed significant inhibition against AChE with an IC50 value in the range of 123.9 ± 10.20 to 342.60 ± 10.60 µM and BuChE in the range of 131.30 ± 9.70 to 375.80 ± 12.80 µM in comparison with standard Donepezil, which has IC50 values of 243.76 ± 5.70 µM (AChE) and 276.60 ± 6.50 µM (BuChE), respectively. Compounds 3, 5 and 9 exhibited potent inhibition against both AChE and BuChE. Molecular docking studies were used to validate and establish the structure–activity relationship of the synthesized derivatives.
ISSN:1424-8247
1424-8247
DOI:10.3390/ph16091278