Compounds > 2-(4-hydroxyphenyl)-4-5-diphenylimidazole

2-(4-hydroxyphenyl)-4-5-diphenylimidazole and Alzheimer-Disease

2-(4-hydroxyphenyl)-4-5-diphenylimidazole has been researched along with Alzheimer-Disease* in 1 studies

Other Studies

1 other study(ies) available for 2-(4-hydroxyphenyl)-4-5-diphenylimidazole and Alzheimer-Disease

Article	Year
In silico studies, synthesis and pharmacological evaluation to explore multi-targeted approach for imidazole analogues as potential cholinesterase inhibitors with neuroprotective role for Alzheimer's disease. Bioorganic & medicinal chemistry, 2018, 05-01, Volume: 26, Issue:8 Alzheimer's disease (AD) is a progressive neurodegenerative disorder with multiple factors associated with its pathogenesis. Our strategy against AD involves design of multi-targeted 2-substituted-4,5-diphenyl-1H-imidazole analogues which can interact and inhibit AChE, thereby, increasing the synaptic availability of ACh, inhibit BuChE, relieve induced oxidative stress and confer a neuroprotective role. Molecular docking was employed to study interactions within the AChE active site. In silico ADME study was performed to estimate pharmacokinetic parameters. Based on computational studies, some analogues were synthesized and subjected to pharmacological evaluation involving antioxidant activity, toxicity and memory model studies in animals followed by detailed mechanistic in vitro cholinesterase inhibition study. Amongst the series, analogue 13 and 20 are the most promising multi-targeted candidates which can potentially increase memory, decrease free radical levels and protect neurons against cognitive deficit. Topics: Acetylcholinesterase; Alzheimer Disease; Animals; Butyrylcholinesterase; Cholinesterase Inhibitors; Disease Models, Animal; Dose-Response Relationship, Drug; Electrophorus; Female; Horses; Imidazoles; Male; Maze Learning; Memory Disorders; Mice; Molecular Structure; Neuroprotective Agents; Structure-Activity Relationship	2018

Article

Year

In silico studies, synthesis and pharmacological evaluation to explore multi-targeted approach for imidazole analogues as potential cholinesterase inhibitors with neuroprotective role for Alzheimer's disease.

Bioorganic & medicinal chemistry, 2018, 05-01, Volume: 26, Issue:8

Alzheimer's disease (AD) is a progressive neurodegenerative disorder with multiple factors associated with its pathogenesis. Our strategy against AD involves design of multi-targeted 2-substituted-4,5-diphenyl-1H-imidazole analogues which can interact and inhibit AChE, thereby, increasing the synaptic availability of ACh, inhibit BuChE, relieve induced oxidative stress and confer a neuroprotective role. Molecular docking was employed to study interactions within the AChE active site. In silico ADME study was performed to estimate pharmacokinetic parameters. Based on computational studies, some analogues were synthesized and subjected to pharmacological evaluation involving antioxidant activity, toxicity and memory model studies in animals followed by detailed mechanistic in vitro cholinesterase inhibition study. Amongst the series, analogue 13 and 20 are the most promising multi-targeted candidates which can potentially increase memory, decrease free radical levels and protect neurons against cognitive deficit.

Topics: Acetylcholinesterase; Alzheimer Disease; Animals; Butyrylcholinesterase; Cholinesterase Inhibitors; Disease Models, Animal; Dose-Response Relationship, Drug; Electrophorus; Female; Horses; Imidazoles; Male; Maze Learning; Memory Disorders; Mice; Molecular Structure; Neuroprotective Agents; Structure-Activity Relationship

2018