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

Molecules

Jan Korabecny¹  Kamil Musilek¹  Ondrej Holas¹  Eugenie Nepovimova¹  Daniel Jun¹  Filip Zemek¹  Veronika Opletalova¹  Jiri Patocka¹  Vlastimil Dohnal¹  Florian Nachon¹  Jana Hroudova¹  Zdenek Fisar¹ 

[1]¹Department of Pharmaceutical Chemistry and Drug Control, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic

关键词: tacrine;    acetylcholinesterase;    butyrylcholinesterase;    7-MEOTA;    inhibition;    Alzheimer disease;   

DOI  :  10.3390/molecules15128804

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.