Substituted spiro [2.3'] oxindolespiro [3.2″]-5,6-dimethoxy-indane-1″-one-pyrrolidine analogue as inhibitors of acetylcholinesterase

Mohamed Ashraf Ali; Rusli Ismail; Tan Soo Choon; Yeong Keng Yoon; Ang Chee Wei; Suresh Pandian; Raju Suresh Kumar; Hasnah Osman; Elumalai Manogaran

doi:10.1016/j.bmcl.2010.09.108

Substituted spiro [2.3'] oxindolespiro [3.2″]-5,6-dimethoxy-indane-1″-one-pyrrolidine analogue as inhibitors of acetylcholinesterase

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7064-6. doi: 10.1016/j.bmcl.2010.09.108. Epub 2010 Sep 26.

Authors

Mohamed Ashraf Ali¹, Rusli Ismail, Tan Soo Choon, Yeong Keng Yoon, Ang Chee Wei, Suresh Pandian, Raju Suresh Kumar, Hasnah Osman, Elumalai Manogaran

Affiliation

¹ Pharmacogenetic and Novel Therapeutics Research, Institute for Research in Molecular Medicine, Universiti Sains Malaysia, Pennag, Malaysia. asraf80med@rediffmail.com

PMID: 20951037
DOI: 10.1016/j.bmcl.2010.09.108

Abstract

Series of pyrolidine analogues were synthesized and examined as acetylcholinesterase (AChE) inhibitors. Among the compounds, compounds 4k and 6k were the most potent inhibitors of the series. Compound 4k, showed potent inhibitory activity against acetyl cholinesterase enzyme with IC(50) 0.10 μmol/L. Pyrolidine analogues might be potential acetyl cholinesterase agents for AD.

MeSH terms

Alzheimer Disease / drug therapy
Cholinesterase Inhibitors / chemistry*
Cholinesterase Inhibitors / pharmacology
Humans
Inhibitory Concentration 50
Molecular Structure
Pyrrolidines / chemical synthesis*
Pyrrolidines / pharmacology*
Spiro Compounds
Structure-Activity Relationship

Substances

Cholinesterase Inhibitors
Pyrrolidines
Spiro Compounds