Korabecny_2015_Molecules_20_22084

Reference

Title : 7-Methoxytacrine-p-Anisidine Hybrids as Novel Dual Binding Site Acetylcholinesterase Inhibitors for Alzheimer's Disease Treatment - Korabecny_2015_Molecules_20_22084
Author(s) : Korabecny J , Andrs M , Nepovimova E , Dolezal R , Babkova K , Horova A , Malinak D , Mezeiova E , Gorecki L , Sepsova V , Hrabinova M , Soukup O , Jun D , Kuca K
Ref : Molecules , 20 :22084 , 2015
Abstract :

Alzheimer's disease (AD) is a debilitating progressive neurodegenerative disorder that ultimately leads to the patient's death. Despite the fact that novel pharmacological approaches endeavoring to block the neurodegenerative process are still emerging, none of them have reached use in clinical practice yet. Thus, palliative treatment represented by acetylcholinesterase inhibitors (AChEIs) and memantine are still the only therapeutics used. Following the multi-target directed ligands (MTDLs) strategy, herein we describe the synthesis, biological evaluation and docking studies for novel 7-methoxytacrine-p-anisidine hybrids designed to purposely target both cholinesterases and the amyloid cascade. Indeed, the novel derivatives proved to be effective non-specific cholinesterase inhibitors showing non-competitive AChE inhibition patterns. This compounds' behavior was confirmed in the subsequent molecular modeling studies.

PubMedSearch : Korabecny_2015_Molecules_20_22084
PubMedID: 26690394

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Citations formats

Korabecny J, Andrs M, Nepovimova E, Dolezal R, Babkova K, Horova A, Malinak D, Mezeiova E, Gorecki L, Sepsova V, Hrabinova M, Soukup O, Jun D, Kuca K (2015)
7-Methoxytacrine-p-Anisidine Hybrids as Novel Dual Binding Site Acetylcholinesterase Inhibitors for Alzheimer's Disease Treatment
Molecules 20 :22084

Korabecny J, Andrs M, Nepovimova E, Dolezal R, Babkova K, Horova A, Malinak D, Mezeiova E, Gorecki L, Sepsova V, Hrabinova M, Soukup O, Jun D, Kuca K (2015)
Molecules 20 :22084