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 |
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| Institution: | 1. Nobel Drug Pharmaceutical R&D Center (Nobel-Ilac Ar-Ge Merkezi), Sancaklar Koyu Mevkii, 81100 Duzce, Turkey;2. Eastern Mediterranean University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Famagusta via Mersin 10, Turkey;1. Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, 2-3-10 Kanda-Surugadai, Chiyoda-ku, Tokyo 101-0062, Japan;2. Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan;1. Alchemical Research, LLC, 260 East Wall Street, Bethlehem, PA 18018, USA;2. Division of Pharmaceutical Sciences, School of Pharmacy, and Department of Chemistry, University of Wisconsin, Madison, WI 53705, USA;1. Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Facultat de Farmàcia, and Institut de Biomedicina (IBUB), Universitat de Barcelona, Av. Joan XXIII 27-31, 08028 Barcelona, Spain;2. Department of Pathogen Molecular Biology, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, United Kingdom;3. Bradford School of Pharmacy, University of Bradford, West Yorkshire BD7 1 DP, United Kingdom;4. Department of Pharmaceutics, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana;5. Departament de Farmacologia, de Terapèutica i de Toxicologia, Universitat Autònoma de Barcelona, 08193-Bellaterra, Barcelona, Spain;1. School of Pharmacy, Health Sciences Campus, University of Waterloo, Waterloo, Ontario, Canada N2L 3G1;2. Department of Chemistry, University of Waterloo, Waterloo, Ontario, Canada N2L 3G1;1. Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia;2. Department of Chemotherapy, Influenza Research Institute, 15/17 Prof. Popova St., 197376 St. Petersburg, Russia;3. Novosibirsk State University, Pirogova 2, Novosibirsk 630090, Russia;1. Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Facultat de Farmàcia, and Institut de Biomedicina (IBUB), Universitat de Barcelona, Av. Joan XXIII, 27-31, E-08028 Barcelona, Spain;3. Nutrition and Food Science Department, XaRTA, INSA, Facultat de Farmàcia, Universitat de Barcelona, Av. Joan XXIII, 27-31, E-08028 Barcelona, Spain;4. CIBER CB06/03 Fisiopatología de la Obesidad y la Nutrición (CIBEROBN), Instituto de Salud Carlos III, Spain;5. Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, CNRS, LabEx LERMIT, 1, Avenue de la Terrasse, 91198 Gyf-sur-Yvette, France;6. Departament de Farmacologia, de Terapèutica i de Toxicologia, Institut de Neurociències, Universitat Autònoma de Barcelona, E-08193 Bellaterra, Barcelona, Spain;7. Departament de Fisicoquímica, Facultat de Farmàcia (Campus Torribera), and IBUB, Universitat de Barcelona, Prat de la Riba 171, E-08921 Santa Coloma de Gramenet, Spain |
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| Abstract: | Hydroxylated 6H-benzoc]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-benzoc]chromen-6-one, and 7,8,9,10-tetrahydro-benzoc]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. |
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| Keywords: | Acetylcholinesterase Butyrylcholinesterase Alzheimer’s Disease Passive avoidance test |
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