alexa Acetylcholinesterase and Butyrylcholinesterase Inhibitory Properties of Functionalized Tetrahydroacridines and Related Analogs
ISSN: 2161-0444

Medicinal Chemistry
Open Access

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Research Article

Acetylcholinesterase and Butyrylcholinesterase Inhibitory Properties of Functionalized Tetrahydroacridines and Related Analogs

Haixiao Jin1, Thuy Nguyen2,3 and Mei-Lin Go3*

1Key Laboratory of Applied Marine Biotechnology, Ministry of Education, School of Marine Sciences, Ningbo University, Ningbo, Fenghua Road 818, Jiangbei District,Zhejiang, 315211, People's Republic of China

2Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, 800E Leigh Street, Richmond, VA 23298-0540, USA

3Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Republic of Singapore 117543

*Corresponding Author:
Mei-Lin Go
Department of Pharmacy
National University of Singapore 18 Science
Drive 4, Republic of Singapore 117543 Singapore
Tel:+65 6516 2654
Fax:+65 6779 1554
E-mail: [email protected]

Received date: August 30, 2014; Accepted date: September 24, 2014; Published date: September 26, 2014

Citation: Jin H, Nguyen T, Mei-Lin G (2014) Acetylcholinesterase and Butyrylcholinesterase Inhibitory Properties of Functionalized Tetrahydroacridines and Related Analogs. Med chem 4:688-696. doi:10.4172/2161-0444.1000213

Copyright: © 2014 Jin H, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

 

Abstract

Functionalized acridines, tetrahydroacridines and quinolines were evaluated for in vitro AChE and BChE inhibitory activities. Potent nanomolar inhibition of both enzymes was found in the tacrine-donepezil hybrid N-(1-benzylpiperidin- 4-yl)-6-chloro-1,2,3,4-tetrahydroacridin-9-amine (51). Molecular modelling and kinetic studies support the notion that 51 occupied the catalytic and peripheral anionic sites of AChE. The physicochemical properties (polar surface area, lipophilicity, hydrogen bonding characteristics) of 51 were within the threshold limits for permeability across the blood brain barrier. Thus, 51 is a promising hybrid inhibitor derived from two established with clinical relevance to neurodegenerative diseases.

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