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Gulcan H.O.,Nobel Drug Pharmaceutical Randnter Nobel Ilac Ar Ge Merkezi | Gulcan H.O.,Eastern Mediterranean University | Unlu S.,Nobel Drug Pharmaceutical Randnter Nobel Ilac Ar Ge Merkezi | Esiringu I.,Nobel Drug Pharmaceutical Randnter Nobel Ilac Ar Ge Merkezi | And 5 more authors.
Bioorganic and Medicinal Chemistry | Year: 2014

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. © 2014 Elsevier Ltd. All rights reserved.

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