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  • Novel multi-targeted agents for Alzheimer's disease: Synthesis, biological evaluation, and molecular modeling of novel 2-[4-(4-substitutedpiperazin-1-yl)phenyl]benzimidazoles.

Novel multi-targeted agents for Alzheimer's disease: Synthesis, biological evaluation, and molecular modeling of novel 2-[4-(4-substitutedpiperazin-1-yl)phenyl]benzimidazoles.

Bioorganic chemistry (2017-05-10)
Keriman Ozadali-Sari, Tuba Tüylü Küçükkılınç, Beyza Ayazgok, Ayla Balkan, Oya Unsal-Tan
ABSTRACT

The present study describes the synthesis, pharmacological evaluation (BChE/AChE inhibition, Aβ antiaggregation, and neuroprotective effects), and molecular modeling studies of novel 2-[4-(4-substitutedpiperazin-1-yl)phenyl]benzimidazole derivatives. The alkyl-substituted derivatives exhibited selective inhibition on BChE with varying efficiency. Compounds 3b and 3d were found to be the most potent inhibitors of BChE with IC

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Butyrylcholinesterase from equine serum, lyophilized powder, ≥900 units/mg protein
Sigma-Aldrich
Amyloid β Protein Fragment 1-40, ≥90% (HPLC), powder