Korabecny_2010_Bioorg.Med.Chem.Lett_20_6093

Reference

Title : Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease - Korabecny_2010_Bioorg.Med.Chem.Lett_20_6093
Author(s) : Korabecny J , Musilek K , Holas O , Binder J , Zemek F , Marek J , Pohanka M , Opletalova V , Dohnal V , Kuca K
Ref : Bioorganic & Medicinal Chemistry Lett , 20 :6093 , 2010
Abstract : All approved drugs for Alzheimer disease (AD) in clinical practice ameliorate the symptoms of the disease. Among them, acetylcholinesterase inhibitors (AChEIs) are used to increase the cholinergic activity. Among new AChEI, tacrine compounds were found to be more toxic compared to 7-MEOTA (9-amino-7-methoxy-1,2,3,4-tetrahydroacridine). In this Letter, series of 7-MEOTA analogues (N-alkyl-7-methoxytacrine) were synthesized. Their inhibitory ability was evaluated on recombinant human acetylcholinesterase (AChE) and plasmatic human butyrylcholinesterase (BChE). Three novel compounds showed promising results towards hAChE better to THA or 7-MEOTA. Three compounds resulted as potent inhibitors of hBChE. The SAR findings highlighted the C(6)-C(7)N-alkyl chains for cholinesterase inhibition.
ESTHER : Korabecny_2010_Bioorg.Med.Chem.Lett_20_6093
PubMedSearch : Korabecny_2010_Bioorg.Med.Chem.Lett_20_6093
PubMedID: 20817518

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Citations formats

Korabecny J, Musilek K, Holas O, Binder J, Zemek F, Marek J, Pohanka M, Opletalova V, Dohnal V, Kuca K (2010)
Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease
Bioorganic & Medicinal Chemistry Lett 20 :6093

Korabecny J, Musilek K, Holas O, Binder J, Zemek F, Marek J, Pohanka M, Opletalova V, Dohnal V, Kuca K (2010)
Bioorganic & Medicinal Chemistry Lett 20 :6093