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Microwave-assisted synthesis and evaluation of anti-inflammatory activity of new series of N-substituted 2-butyl-5-chloro-3H-imidazole-4-carbaldehyde derivatives

Evaluation of a new lead for acetylcholinesterase inhibition

Medicinal Chemistry Research : Volume 18, Issue 1, February 2009

Medicinal Chemistry Research : Volume 17

Medicinal Chemistry Research : Volume 16

Medicinal Chemistry Research : Volume 15

Medicinal Chemistry Research : Volume 14

Medicinal Chemistry Research : Volume 13

Evaluation of a new lead for acetylcholinesterase inhibition

Content Provider	Springer Nature Link
Author	Khorana, Nantaka Markmee, Sutthatip Ingkaninan, Kornkak Ruchirawat, Somsak Kitbunnadaj, Ruengwit Pullagurla, Manik Reddy
Copyright Year	2008
Abstract	Acetylcholine is the most common neurotransmitter of the parasympathetic nervous system. Several cholinergic drugs are widely used in Alzheimer’s disease, urinary retention, glaucoma, and myasthenia gravis. Acetylcholinesterase is the enzyme which destroys naturally occurring acetylcholine, and acetylcholinesterase inhibitors (AChEIs) which block the enzyme are currently used in the treatment of several diseases, most importantly Alzheimer’s disease. Previous studies from our laboratory have shown a few isoquinoline analogs to be potential acetylcholinesterase inhibitors. In the present study we have extended analysis of the structure–activity relationship (SAR) of the isoquinoline ring system as an AChEI. The corresponding reduced form of 1-(3,4-dimethoxybenzyl)-6,7-dimethoxyisoquinoline, ring-opened analog, and related analogs were evaluated for AChE inhibitory activity. Our results showed that the dihydroisoquinoline ring analog compound 6 (IC50 = 7.0 ± 1.4 μM) and compound 4 (IC50 = 5.5 ± 1.0 μM) displayed potent AChE inhibition. These compounds are currently the lead compounds for further studies in our laboratory.
Starting Page	231
Ending Page	241
Page Count	11
File Format	PDF
ISSN	10542523
Journal	Medicinal Chemistry Research
Volume Number	18
Issue Number	3
e-ISSN	15548120
Language	English
Publisher	SP Birkhäuser Verlag Boston
Publisher Date	2008-08-15
Publisher Place	Boston
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Acetylcholinesterase inhibitor Butyrylcholinesterase inhibitor Isoquinoline analogs Synthesis Cell Biology Biochemistry Pharmacology/Toxicology
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology, Toxicology and Pharmaceutics

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