Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 119, Issue -, Pages 260-277Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.04.053
Keywords
Alzheimer's disease; Acetylcholinesterase; Triazolopyrimidine; Quinoline; Molecular docking; Butyrylcholinesterase
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Funding
- CSIR (New Delhi)
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In present study a series of triazolopyrimidine-quinoline and cyanopyridine-quinoline hybrids were designed, synthesized and evaluated as acetylcholinesterase inhibitors (AChEIs). Molecular docking and scoring was utilized for the design of inhibitors. The molecules were synthesized via an easily accessible, convergent synthetic route. Three triazolopyrimidine based compounds showed nanomolar activity towards acetylcholinesterase. Among them, Ethyl 6-fluoro-4-(4-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperazin-1-yl)quinoline-3-carboxylate (10d), strongly inhibited AChE with IC50 value of 42 nM. Furthermore compound 10d was identified as most promising compound with 12 fold selectivity against butyrylcholinesterase (BuChE). This compound displayed a composed multitargeted profile with promising inhibition of self-induced and AChE - induced A beta aggregation and antioxidant activity. (C) 2016 Elsevier Masson SAS. All rights reserved.
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