Substituted cinnamic anhydrides act as selective inhibitors of acetylcholinesterase |
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| Affiliation: | 1. Université Paris-Saclay, CNRS, Institut de Chimie des Substances Naturelles, UPR 2301, 91198 Gif-sur-Yvette, France;2. Department of Chemistry, Faculty of Science, University of Malaya, 50603 Kuala Lumpur, Malaysia;3. Université Paris-Saclay, UMR CNRS 8126, Institut Gustave Roussy, 114 rue Edouard-Vaillant, 94805 Villejuif Cedex, France;4. Université Paris-Saclay, BioCIS, Faculté de Pharmacie de Châtenay-Malabry, 5 rue Jean-Baptiste Clément, 92296 Châtenay-Malabry, France;5. Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia;1. Natural and Medical Sciences Research Center, University of Nizwa, P.O. Box 33, Postal Code 616, Birkat Al Mauz, Nizwa, Oman;2. Organic Chemistry, Martin-Luther-University Halle-Wittenberg, Kurt-Mothes-Str. 2, d-06120 Halle (Saale), Germany;1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Kafrelsheikh University, Kafrelsheikh, Egypt;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Egyptian Russian University, Badr City, Cairo 11829, Egypt;3. Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Polo Scientifico, Via U. Schiff 6, 50019, Sesto Fiorentino, Firenze, Italy;4. Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, Laboratory of Molecular Modeling Cheminformatics & QSAR, University of Florence, Polo Scientifico, Via U. Schiff 6, 50019, Sesto Fiorentino, Firenze, Italy;5. Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia;6. Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt;1. Endocannabinoid Research Group, Institute of Biomolecular Chemistry, National Research Council, Via Campi Flegrei 34, Comprensorio Olivetti, 80078 Pozzuoli, Naples, Italy;2. Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza—Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy;3. Department of Chemistry and Biochemistry, North Dakota State University, Fargo, ND 58108, United States;4. Department of Chemistry, University of Wisconsin-River Falls, 410 S. Third St., River Falls, WI 54022, United States;1. Department of Chemistry, Quaid-I-Azam University, Islamabad 45320, Pakistan;2. Centre for Advanced Drug Research, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan;3. Institute of Biomedical and Genetic Engineering, PO Box 2891, Sector G-9/1, Islamabad, Pakistan;4. Department of Bioinformatics, Fraunhofer Institute SCAI, Sankt Augustin, Germany;5. Department of Pharmaceutical Sciences, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan |
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| Abstract: | Cinnamic anhydrides have been shown to be more than reactive reagents, but they also act as inhibitors of the enzyme acetylcholinesterease (AChE). Thus, out of a set of 33 synthesised derivatives, several of them were mixed type inhibitors for AChE (from electric eel). Thus, (E)-3-(2,4-dimethoxyphenyl)acrylic anhydride (2c) showed Ki = 8.30 ± 0.94 µM and Ki′ = 9.54 ± 0.38 µM, and for (E)-3-(3-chlorophenyl)acrylic anhydride (2u) Ki = 8.23 ± 0.93 µM and Ki′ = 13.07 ± 0.46 µM were measured. While being not cytotoxic to many human cell lines, these compounds showed an unprecedented and noteworthy inhibitory effect for AChE but not for butyrylcholinesterase (BChE). |
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| Keywords: | Cinnamic anhydrides Acetylcholinesterase Butyrylcholinesterase Inhibitors |
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