Back to Search Start Over

Synthesis and In Vitro Evaluation of N-(Bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine as a Cholinesterase Inhibitor with Regard to Alzheimer's Disease Treatment

Authors :
Jiri Patocka
Jan Korabecny
Kamil Kuca
Zdenek Fisar
Jana Hroudova
Florian Nachon
Vlastimil Dohnal
Filip Zemek
Veronika Opletalova
Daniel Jun
Eugenie Nepovimova
Ondrej Holas
Kamil Musilek
Source :
Molecules, Vol 15, Iss 12, Pp 8804-8812 (2010)
Publication Year :
2010
Publisher :
MDPI AG, 2010.

Abstract

A new tacrine based cholinesterase inhibitor, N-(bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine (1), was designed and synthesized to interact with specific regions of human acetylcholinesterase and human butyrylcholinesterase. Its inhibitory ability towards cholinesterases was determined and compared to tacrine (THA) and 9-amino-7-methoxy-1,2,3,4-tetrahydroacridine (7-MEOTA). The assessment of IC50 values revealed 1 as a weak inhibitor of both tested enzymes.

Details

Language :
English
ISSN :
14203049
Volume :
15
Issue :
12
Database :
Directory of Open Access Journals
Journal :
Molecules
Publication Type :
Academic Journal
Accession number :
edsdoj.47589d8844599b46912943b1405e5
Document Type :
article
Full Text :
https://doi.org/10.3390/molecules15128804