TITLE

An Overview of the Current and Novel Drugs for Alzheimer's Disease with Particular Reference to Anti-Cholinesterase Compounds

AUTHOR(S)
Colombres, Marcela; Sagal, Juan Paulo; Inestrosa, Nibaldo C.
PUB. DATE
September 2004
SOURCE
Current Pharmaceutical Design;Oct2004, Vol. 10 Issue 25, p3121
SOURCE TYPE
Academic Journal
DOC. TYPE
Article
ABSTRACT
Several cellular processes could be targeted if the complex nature of Alzheimer' s disease (AD) was already understood. Most of AD treatments have been focused on the inhibition of acetylcholinesterase (AChE) in order to raise the levels of its substrate, i.e. the neurotransmitter acetylcholine (ACh), to augment cognitive functions of affected patients. Effectiveness in AChE inhibition and side-effect issues of clinical (tacrine, donepezil, galanthamine and rivastigmine) as well as of novel inhibitors is reviewed here. Novel design methods for the inhibition of AChE include the use of in silico tools to predict the interactions between AChE and the desired compound, both at the active site of the enzyme, responsible of hydroly sing ACh and with the peripheral anionic site (PAS), which has been described as a promoting agent of the amyloid �-peptide (A�) aggregation present in the senile plaques of the brain of AD individuals.
ACCESSION #
14545998

 

Related Articles

  • Synthesis and In Vitro Evaluation of N-(Bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine as a Cholinesterase Inhibitor with Regard to Alzheimer's Disease Treatment. Korabecny, Jan; Musilek, Kamil; Holas, Ondrej; Nepovimova, Eugenie; Jun, Daniel; Zemek, Filip; Opletalova, Veronika; Patocka, Jiri; Dohnal, Vlastimil; Nachon, Florian; Hroudova, Jana; Fisar, Zdenek; Kuca, Kamil // Molecules;Dec2010, Vol. 15 Issue 12, p8804 

    A new tacrine based cholinesterase inhibitor, N-(bromobut-3-en-2-yl)-7- methoxy-1,2,3,4-tetrahydroacridin-9-amine (1), was designed and synthesized to interact with specific regions of human acetylcholinesterase and human butyrylcholinesterase. Its inhibitory ability towards cholinesterases was...

  • Potential inhibitors against acetylcholinesterase and glutathione S-transferase associated with alzheimer's disease. Lalwani, Atul; Paul, Somdeb; Ahmed, Iliazuddin; Ramanathan, K. // Journal of Chemical & Pharmaceutical Research;2014, Vol. 6 Issue 3, p1527 

    Cholinesterase inhibitors are employed as the standard therapeutic approach for the treatment of Alzheimer's disease (AD). Cheminformatics tools such as CORINA, Yet Another Scientific Artificial Reality Application (YASARA), JME molecular editor and molecular docking program are employed to...

  • Flavanone Glycosides as Acetylcholinesterase Inhibitors: Computational and Experimental Evidence. REMYA, C.; DILEEP, K. V.; TINTU, I.; VARIYAR, E. J.; SADASIVAN, C. // Indian Journal of Pharmaceutical Sciences;Nov/Dec2014, Vol. 76 Issue 6, p567 

    Acetylcholinesterase hydrolyzes the neurotransmitter called acetylcholine and is crucially involved in the regulation of neurotransmission. One of the observable facts in the neurodegenerative disorders like Alzheimer's disease is the decrease in the level of acetylcholine. Available drugs that...

  • Disease progression and costs of care in Alzheimer's disease patients treated with donepezil: a longitudinal naturalistic cohort. Gustavsson, Anders; Jönsson, Linus; Parmler, Johan; Andreasen, Niels; Wattmo, Carina; Wallin, Åsa; Minthon, Lennart // European Journal of Health Economics;Oct2012, Vol. 13 Issue 5, p561 

    Background/Aims: Improved data and methods are needed for modeling disease progression in Alzheimer's disease (AD) for economic evaluation of treatments. The aim is to estimate prediction models for long-term AD progression and subsequently economic outcomes. Methods: Three-year follow-up data...

  • Cholinesterase inhibitors. Lee, Philip E.; Hsiung, Ging-Yuek Robin; Seitz, Dallas; Gill, Sudeep S.; Rochon, Paula A. // British Columbia Medical Journal;Oct2011, Vol. 53 Issue 8, p404 

    Cholinesterase inhibitors are the most common medications used for the symptomatic treatment of Alzheimer disease. Data from published clinical trials have shown benefits for cognitive, behavioral, and functional outcomes. While the overall effect size identified in the trials is small, clinical...

  • acetylcholine.  // Royal Society of Medicine: Medicines;2002, p29 

    This article presents information on acetylcholine drug which is a neurotransmitter in the body. It has a number of important roles in both the central and peripheral nervous systems, relaying messages between nerves or from nerves to innervated organs. In medicine, it is rarely used as a drug...

  • Natural Products and their Derivatives as Cholinesterase Inhibitors in the Treatment of Neurodegenerative Disorders: An Update. Loizzo, Monica Rosa; Tundis, Rosa; Menichini, Federica; Menichini, Francesco // Current Medicinal Chemistry;2008, Vol. 15 Issue 12, p1209 

    Alzheimer's disease (AD) is the most common form of neurodegenerative disorders. If more effective therapies than the ones currently available are not developed that either prevent AD or other neurodegenerative or block progression of the diseases in its very early stages, the economic and...

  • Steady-State Pharmacokinetics of Rivastigmine in Patients with Mild to Moderate Alzheimer's Disease Not Affected by Co-Administration of Memantine: An Open-Label, Crossover, Single-Centre Study. Shua-Haim, Joshua; Smith, Juanita; Picard, Franck; Sedek, Greg; Athalye, Sandeep; Pommier, Françoise; Lefèvre, Gilbert // Clinical Drug Investigation;2008, Vol. 28 Issue 6, p361 

    Background and objective: It has been shown that combining memantine and a cholinesterase inhibitor, which each affect different neurotransmitter systems, may offer further improvements in efficacy over either treatment alone in patients with Alzheimer's disease. The present study was conducted...

  • An Overview on Natural Cholinesterase Inhibitors - A Multi-Targeted Drug Class - and Their Mass Production. Orhan, I. Erdogan; Orhan, G.; Gurkas, E. // Mini Reviews in Medicinal Chemistry;Sep2011, Vol. 11 Issue 10, p836 

    Cholinesterase enzyme family consisting of acetylcholinesterase (AChE) and butrylcholinesterase (BChE) is important in pathogenesis of Alzheimer's disease (AD), explained by "cholinergic hypothesis". Accordingly, deficiency of the neuromediator called "acetylcholine" excessive amount of BChE has...

Share

Read the Article

Courtesy of THE LIBRARY OF VIRGINIA

Sorry, but this item is not currently available from your library.

Try another library?
Sign out of this library

Other Topics