Title : 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 - Korabecny_2010_Molecules_15_8804 |
Author(s) : Korabecny J , Musilek K , Holas O , Nepovimova E , Jun D , Zemek F , Opletalova V , Patocka J , Dohnal V , Nachon F , Hroudova J , Fisar Z , Kuca K |
Ref : Molecules , 15 :8804 , 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. |
PubMedSearch : Korabecny_2010_Molecules_15_8804 |
PubMedID: 21127466 |
Korabecny J, Musilek K, Holas O, Nepovimova E, Jun D, Zemek F, Opletalova V, Patocka J, Dohnal V, Nachon F, Hroudova J, Fisar Z, Kuca K (2010)
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
15 :8804
Korabecny J, Musilek K, Holas O, Nepovimova E, Jun D, Zemek F, Opletalova V, Patocka J, Dohnal V, Nachon F, Hroudova J, Fisar Z, Kuca K (2010)
Molecules
15 :8804