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A new series of tacrine-coumarin hybrids linked to 1,2,3-triazole were designed, synthesized, and tested as potent dual binding site cholinesterase inhibitors (ChEIs) for the treatment of Alzheimer's disease (AD). Among them, compound 8e was the most potent anti-AChE derivative (IC = 27 nM) and compound 8m displayed the best anti-BChE activity (IC = 6 nM) much more active than tacrine and donepezil as the reference drugs. Compound 8e was also evaluated for its BACE1 inhibitory activity and neuroprotectivity against PC12 cells exposed to Aβ which indicated low activity. Finally, in vivo studies by Morris water maze task showed that compound 8e significantly reversed scopolamine-induced memory deficit in rats.
This article was published in the following journal.
Name: Bioorganic chemistry
Bacterial infections, caused predominately by Gram-positive and Gram-negative organisms, are proliferation of harmful strains of bacteria on or inside the body. Hospital-acquired and community-acquire...
Structurally diverse trimethoxyphenyl-1,2,3-triazole hybrids were designed, synthesized and evaluated for their antiproliferative activity against three cancer cell lines (PC3, MGC803 and HepG2). Amon...
Alzheimer's disease (AD) is a severe age-dependent neurodegenerative disorder affecting several million people worldwide. So far, there is no adequate medication to prevent or slow down the progressio...
Both cholinesterases (AChE and BChE) and kinases, such as GSK-3α/β, are associated with the pathology of Alzheimer's disease. Two scaffolds, targeting AChE (tacrine) and GSK-3α/β (valmerin) simult...
Neuroinflammation and cholinergic deficit are key detrimental processes involved in Alzheimer's disease. Hence, in the search for novel and effective treatment strategies, the multi-target-directed li...
Anti-viral therapy in Alzheimer's disease will investigate the efficacy of treating patients with mild Alzheimer's disease with the U.S.A marketed generic anti-viral drug Valtrex (valacycl...
The purpose of this study is to determine whether the anti-inflammatory drug celecoxib can delay the onset of Alzheimer Disease (AD) in people with Age Associated Memory Impairment (AAMI)....
This is a randomized controlled trial to develop and test the efficacy of a multi-domain lifestyle behavioral intervention designed to promote healthier lifestyle behaviors linked to lower...
This project will provide new data to address an important question linking Alzheimer's disease neuropathology to physical disability.
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A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.
Vaccines or candidate vaccines used to prevent or treat ALZHEIMER DISEASE.
A cytostatic triazole derivative which is not to be confused with guanazolo, the generic name for 8-azaguanine.
Triazole antifungal agent that is used to treat oropharyngeal candidiasis and cryptococcal meningitis in AIDS.
A triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.
Neurology - Central Nervous System (CNS)
Alzheimer's Disease Anesthesia Anxiety Disorders Autism Bipolar Disorders Dementia Epilepsy Multiple Sclerosis (MS) Neurology Pain Parkinson's Disease Sleep Disorders Neurology is the branch of me...
Biological therapy involves the use of living organisms, substances derived from living organisms, or laboratory-produced versions of such substances to treat disease. Some biological therapies for cancer use vaccines or bacteria to stimulate the body&rs...