药物化学

Alzheimer Diseases: Substituted Spiro [2.3′] Oxindolespiro [3.2″]-5, 6-Dimethoxy-Indane-1″-One- Indolizine Analogue as Inhibitors of Acetylcholinesterase

Abstract

Mohamed Ashraf Ali, Rusli Ismail, Tan Soo Choon, Raju Suresh Kumar, Mohammad Asad, Abdulrahman I.Almansour, Yeong Keng Yoon, Ang Chee Wei, Karthikeyan Elumalai and Suresh Pandian

Indanone derivatives share vital pharmacological properties, considered useful in alzheimer’s disease (AD).The aim of this study was synthesis and evaluate indolizine analogues if possess acetyl cholinesterase (AChE)inhibitory activity. The easily accessible three-step synthesis of these compounds resulted to be significantly less difficult and expensive than that of donepezil. Several compounds possess anti-cholinesterase activity in the order of micro and sub-micromolar. Particularly, compound 3k was the most potent inhibitors of the series. Compound 3k, showed potent inhibitory activity against acetyl cholinesterase enzyme with IC50 0.10 μmol/L. Indolizine analogues might be potential acetyl cholinesterase agents for AD.