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Novel Tacrine Analogs as Potential Cholinesterase Inhibitors in Alzheimer's Disease
Author(s) -
ElMalah Afaf,
Gedawy Ehab M.,
Kassab Asmaa E.,
Salam Rania M. Abdel
Publication year - 2014
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201300121
Subject(s) - tacrine , acetylcholinesterase , cholinesterase , pharmacology , chemistry , drug , aché , alzheimer's disease , disease , enzyme , medicine , biochemistry
Acetylcholinesterase inhibitors (AChEIs) are used for the treatment of Alzheimer's disease (AD). The increase in ACh levels ameliorates the symptoms of the disease. Tacrine is the first clinically approved drug as AChEI used in the treatment of AD. In this paper, we synthesized new tacrine analogs to act on catalytic and peripheral sites of AChE. Their inhibitory activity was evaluated. All novel compounds except 7a showed promising results toward AChE. Two compounds, 10b and 11b , are more potent than tacrine. Furthermore, molecular‐modeling studies were performed for these two compounds to rationalize the obtained pharmacological activity. Moreover, various drug‐likeness properties of the new compounds were predicted.