Synthesis and pharmacological evaluation of some quinoline derivatives as potential cognition enhancers

Poonam Piplani; Anita Rani; Ruchika Saihgal; Meenakshi Sharma

doi:10.1055/s-0031-1296213

Arzneimittelforschung, Inhaltsverzeichnis

Arzneimittelforschung 2011; 61(7): 373-378
DOI: 10.1055/s-0031-1296213

CNS-active Drugs · Hypnotics · Psychotropics · Sedatives

Editio Cantor Verlag Aulendorf (Germany)

Synthesis and pharmacological evaluation of some quinoline derivatives as potential cognition enhancers

Autoren

Poonam Piplani

¹University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India
Anita Rani

¹University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India
Ruchika Saihgal

¹University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India
Meenakshi Sharma

¹University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India

Abstract

The present paper describes the synthesis of a series of substituted 6-amino (1 a–c) and 8-aminoquinoline derivatives (2b–c) and the evaluation of their ability to prevent the memory decline using a behavioural model, i. e. the elevated plus maze test. The effect of the candidate drugs on the activity of acetylcholinesterase was studied using the enzyme source from the mouse brain. The structures of the synthesized compounds were confirmed by UV, IR, ¹H-NMR and elemental analysis. The 6-aminoquinoline derivative [6-(4-pyridyl)methylaminoquinoline] (1 c) oxalate showed maximum % retention (50% at 5 mg/kg and 75% at 10 mg/kg) in the elevated plus maze test and maximum% inhibition (71% at 25 µM) of AChE on biochemical evaluation.

Key words

Acetycholinesterase - 6-Aminoquinolines - 8-Aminoquinolines - Cogniton enhancers - Elevated plus maze - Quinolines

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Referenzen

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