Synthesis, crystal structure and cholinesterase enzymes inhibitory activities of new pyridine alkaloid derivative

Ghalib, Gaza Murad and Hashim, Rokiah and Mehdi, Sayed Hasan and Da Silva, M. Fátima C. Guedes and Sulaiman, Othman and How, Fiona Ni Foong and Kawamura, Fumio and Jawad, Ali and Algamal, Yousif and Chan, Kit-Lam and Murugaiyah, Vikneswaran (2015) Synthesis, crystal structure and cholinesterase enzymes inhibitory activities of new pyridine alkaloid derivative. Asian Journal of Chemistry, 27 (11). pp. 4092-4096. ISSN 0970-7077 E-ISSN 0975-427X

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Abstract

A new pyridine alkaloid derivative named as 2-(6-benzyl-4-oxo-5-phenyl-1,4-dihydro pyridine-3-yl)-benzoic acid ethylester (3) has been prepared by the reaction of ninhydrin with 1,3-diphenylacetonep-tosylhydrazone and the structure has been established with the help of spectral analysis and X-ray analysis. The title compound demonstrated potent inhibitory activity against butyrylcholinesterase (BChE; IC50 = 4.91 µM) comparable to physostigmine (IC50 = 4.72 x 10-1 µM). However it showed moderate inhibitory activity against acetylcholinesterase (AChE; IC50 = 82.00 µM)). It was BChE selective over AChE, in contrast to physostigmine, which was more AChE selective. Being a potent and selective BChE inhibitor, it may serve as a new class of drug for prevention of the progression of neurodegeneration as well for symptomatic treatment of Alzheimer patient.

Item Type:	Article (Journal)
Additional Information:	6467/46444
Uncontrolled Keywords:	Pyridine alkaloid, Acetylcholinesterase, Butyrylcholinesterase
Subjects:	Q Science > QD Chemistry
Kulliyyahs/Centres/Divisions/Institutes (Can select more than one option. Press CONTROL button):	Kulliyyah of Science > Department of Chemistry
Depositing User:	Dr Fiona How
Date Deposited:	19 Feb 2016 11:39
Last Modified:	21 Aug 2017 11:33
URI:	http://irep.iium.edu.my/id/eprint/46444

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