Results
Title

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

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

Abstract

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.

Subjects

SCHIFF bases; ALZHEIMER'S disease; BENZIMIDAZOLES; SCHIFF base derivatives; MOLECULAR docking; STRUCTURE-activity relationships

Publication

Pharmaceuticals (14248247), 2023, Vol 16, Issue 9, p1278

ISSN

1424-8247

Publication type

Academic Journal

DOI

10.3390/ph16091278