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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
초록

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