Synthesis and discovery of novel hexacyclic cage compounds as inhibitors of acetylcholinesterase

Hexacyclic derivatives share vital pharmacological properties, considered useful in Alzheimer’s disease. The aim of this study was synthesis and its evaluation for acetyl cholinesterase inhibitory activity of novel hexacyclic analogues. Compound 4f, showed potent inhibitory activity against acetyl c...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-07, Vol.21 (13), p.3997-4000
Hauptverfasser:	Suresh Kumar, Raju, Ashraf Ali, Mohamed, Osman, Hasnah, Ismail, Rusli, Choon, Tan Soo, Yoon, Yeong Keng, Wei, Ang Chee, Pandian, Suresh, Manogaran, Elumalai
Format:	Artikel
Sprache:	eng
Schlagworte:	acetylcholinesterase Acetylcholinesterase - chemistry Alzheimer disease Biological and medical sciences cholinesterase Cholinesterase Inhibitors - chemical synthesis Cholinesterase Inhibitors - chemistry Cholinesterase Inhibitors - pharmacology Drug Discovery Heterocyclic Compounds, 4 or More Rings - chemical synthesis Heterocyclic Compounds, 4 or More Rings - chemistry Heterocyclic Compounds, 4 or More Rings - pharmacology Humans Inhibitory Concentration 50 Medical sciences Molecular Structure Neuropharmacology Pharmacology. Drug treatments Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) Psychology. Psychoanalysis. Psychiatry Psychopharmacology
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Zusammenfassung:	Hexacyclic derivatives share vital pharmacological properties, considered useful in Alzheimer’s disease. The aim of this study was synthesis and its evaluation for acetyl cholinesterase inhibitory activity of novel hexacyclic analogues. Compound 4f, showed potent inhibitory activity against acetyl cholinesterase enzyme with IC₅₀ 0.72μmol/L.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.05.003