1622846-97-2Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel 6H-benzo[c]chromen-6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives as potential cholinesterase inhibitors
Gulcan, Hayrettin Ozan,Unlu, Serdar,Esiringu, Ilker,Ercetin, Tugba,Sahin, Yasemin,Oz, Demet,Sahin, Mustafa Fethi
, p. 5141 - 5154 (2015/02/19)
Hydroxylated 6H-benzo[c]chromen-6-one derivatives (i.e., urolithins) are the main bioavailable metabolites, and biomarkers of ellagitannins present in various nutrition. Although these dietaries, the sources of urolithins, are employed in folk medicine as cognitive enhancer in the treatment of Alzheimer's Disease, urolithins have negligible potential to inhibit acetylcholinesterase and butyrylcholinesterase enzymes, the validated targets of Alzheimer's Disease. Therefore, within this research, a series of 6H-benzo[c]chromen-6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives has been designed, synthesized, and their biological activities were evaluated as potential acetylcholinesterase and butyrylcholinesterase inhibitors. The compounds synthesized exerted comparable activity in comparison to rivastigmine, galantamine, and donepezil both in in vitro and in vivo studies.
3-SUBSTITUTED-6H-BENZO[C]CHROMEN-6-ONES AND 3-SUBSTITUTED-7,8,9,10-TETRAHYDRO-6H-BENZO[C]CHROMEN-6-ONES AGAINST SENILE DEMENTIA
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Page/Page column 16; 26-27, (2014/09/03)
This invention is related with the conversion of xenobiotics to potent ACHE and BCHE inhibitors that have activity comparable to the current ACHE and BCHE inhibitor drugs (i.e., donepezil, rivastigmine, and galantamine).
