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Novel tacrine analogs as potential cholinesterase inhibitors in Alzheimer's disease.
Arch Pharm (Weinheim). 2014 Feb; 347(2):96-103.AP

Abstract

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.

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Publisher Full Text (DOI)

Authors+Show Affiliations

El-Malah A
Faculty of Pharmacy, Pharmaceutical Organic Chemistry Department, Cairo University, Cairo, Egypt.
Gedawy EM
No affiliation info available
Kassab AE
No affiliation info available
Salam RM
No affiliation info available

MeSH

AcetylcholinesteraseAlzheimer DiseaseAnimalsCholinesterase InhibitorsDrug DesignElectrophorusHumansMolecular Docking SimulationMolecular StructureStructure-Activity RelationshipTacrine

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

24343873

Citation

El-Malah, Afaf, et al. "Novel Tacrine Analogs as Potential Cholinesterase Inhibitors in Alzheimer's Disease." Archiv Der Pharmazie, vol. 347, no. 2, 2014, pp. 96-103.
El-Malah A, Gedawy EM, Kassab AE, et al. Novel tacrine analogs as potential cholinesterase inhibitors in Alzheimer's disease. Arch Pharm (Weinheim). 2014;347(2):96-103.
El-Malah, A., Gedawy, E. M., Kassab, A. E., & Salam, R. M. (2014). Novel tacrine analogs as potential cholinesterase inhibitors in Alzheimer's disease. Archiv Der Pharmazie, 347(2), 96-103. https://doi.org/10.1002/ardp.201300121
El-Malah A, et al. Novel Tacrine Analogs as Potential Cholinesterase Inhibitors in Alzheimer's Disease. Arch Pharm (Weinheim). 2014;347(2):96-103. PubMed PMID: 24343873.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Novel tacrine analogs as potential cholinesterase inhibitors in Alzheimer's disease. AU - El-Malah,Afaf, AU - Gedawy,Ehab M, AU - Kassab,Asmaa E, AU - Salam,Rania M Abdel, Y1 - 2013/12/16/ PY - 2013/05/01/received PY - 2013/09/08/revised PY - 2013/09/17/accepted PY - 2013/12/18/entrez PY - 2013/12/18/pubmed PY - 2014/7/16/medline KW - Acetylcholinesterase KW - Alzheimer's disease KW - Drug-likeness KW - Molecular-modeling KW - Tacrine SP - 96 EP - 103 JF - Archiv der Pharmazie JO - Arch Pharm (Weinheim) VL - 347 IS - 2 N2 - 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. SN - 1521-4184 UR - https://www.unboundmedicine.com/medline/citation/24343873/Novel_tacrine_analogs_as_potential_cholinesterase_inhibitors_in_Alzheimer's_disease_ DB - PRIME DP - Unbound Medicine ER -