Abstract
Synthesis, Docking and Evaluation of Novel Pyrazole Carboxamide Derivatives as Multifunctional Anti-Alzheimer's Agents
Highlights
Alzheimer’s disease (AD), the most common form of dementia in elderly people, is a complex age-dependent neurodegenerative disorder of the central nervous system, characterized by progressive impairment in memory, cognitive functions, and behavioral disturbances[1]
Another potential therapy for AD is the use of monoamine oxidase-B (MAO-B) inhibitors, as MAO-B type activity is increased in patients with AD[5]
All the compounds significantly decreased the AChE activity in brain as compared to control. These results suggest that pyrazole derivatives due to their anti-AChE activity enhance cholinergic neurotransmission in brain and enhance learning and memory functions
Summary
Alzheimer’s disease (AD), the most common form of dementia in elderly people, is a complex age-dependent neurodegenerative disorder of the central nervous system, characterized by progressive impairment in memory, cognitive functions, and behavioral disturbances[1]. Acetylcholinesterase (AChE) controls acetylcholine to proper levels by degradation; excessive AChE activity leads to constant acetylcholine deficiency, memory, and cognitive impairments This observation led to the development of AChE inhibitors as possible therapy for the loss of cognitive function[3,4]. There are different recognized mechanisms by which MAO-B inhibitors could prevent neurodegeneration They may decrease the free radical formation, which cause membrane and DNA destruction, from normal metabolism of the biogenic amines by inhibition of MAO-B in the central nervous systems. They exhibit protective effects against neuronal apoptosis in cell culture. These findings urged the scientists to synthesize various pyrazole derivatives as MAO-B inhibitors and a significant number of pyrazole derivatives were found to have MAO-B inhibitory activity comparable to or higher than the reference
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