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Title: Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer's disease
Authors: Supatra Thiratmatrakul
Chavi Yenjai
Pornthip Waiwut
Opa Vajragupta
Prasert Reubroycharoen
Michihisa Tohda
Chantana Boonyarat
Khon Kaen University
Ubon Rajathanee University
Mahidol University
Chulalongkorn University
University of Toyama
Keywords: Chemistry;Pharmacology, Toxicology and Pharmaceutics
Issue Date: 21-Mar-2014
Citation: European Journal of Medicinal Chemistry. Vol.75, (2014), 21-30
Abstract: New tacrine-carbazole hybrids were developed as potential multifunctional anti-Alzheimer agents for their cholinesterase inhibitory and radical scavenging activities. The developed compounds showed high inhibitory activity on acetylcholinesterase (AChE) with IC50values ranging from 0.48 to 1.03 μM and exhibited good inhibition selectivity against AChE over butyrylcholinesterase (BuChE). Molecular modeling studies revealed that these tacrine-carbazole hybrids interacted simultaneously with the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. The derivatives containing methoxy group showed potent ABTS radical scavenging activity. Considering their neuroprotection, our results indicate that these derivatives can reduce neuronal death induced by oxidative stress and β-amyloid (Aβ). Moreover, S1, the highest potency for both radical scavenging and AChE inhibitory activity, exhibited an ability to improve both short-term and long-term memory deficit in mice induced by scopolamine. Overall, tacrine-carbazole derivatives can be considered as a candidate with potential impact for further pharmacological development in Alzheimer's therapy. © 2014 Elsevier Masson SAS. All rights reserved.
ISSN: 17683254
Appears in Collections:Scopus 2011-2015

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