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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

Bioorganic and Medicinal Chemistry · Ekim 2014

Makale Bilgileri

DergiBioorganic and Medicinal Chemistry
Yayın TarihiEkim 2014
Cilt / Sayfa22 · 5141-5154
Özet 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.

Yazarlar (7)

1
Hayrettin Ozan Gulcan
2
Serdar Ünlü
3
Ilker Esiringu
4
Tugba Ercetin
5
Yasemin Şahin
6
Demet Öz
7
Mustafa Şahin

Anahtar Kelimeler

6H-Benzo[c]chromen-6-ones Acetylcholinesterase Alzheimer's Disease Butyrylcholinesterase Passive avoidance test

Kurumlar

Eastern Mediterranean University
Famagusta Turkey
Nobel Drug Pharmaceutical RandD Center (Nobel-Ilac Ar-Ge Merkezi)
Turkey

Metrikler

42
Atıf
7
Yazar
5
Anahtar Kelime

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