296791-59-8Relevant academic research and scientific papers
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
Gurjar, Archana S.,Darekar, Mrunali N.,Yeong, Keng Yoon,Ooi, Luyi
, p. 1511 - 1522 (2018)
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.
A simple and straightforward method for one-pot synthesis of 2,4,5-triarylimidazoles using titanium dioxide as an eco-friendly and recyclable catalyst under solvent-free conditions
Brahmachari, Goutam,Das, Suvankar
, p. 387 - 393 (2013/05/08)
Titanium dioxide has been found to be a mild and effective catalyst for the straightforward and efficient synthesis of 2,4,5-triarylimidazoles by three-component, one-pot condensation of 1,2-diketones, aryl aldehydes and ammonium acetate under solvent-free conditions. The operational simplicity, good yield of products, and the use of non-toxic, inexpensive and recyclable heterogeneous catalyst makes this environmentally benign three-component one-pot cyclo-condensation reaction as an attractive method.
