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https://hdl.handle.net/11499/10852| Title: | Synthesis of novel acridine-sulfonamide hybrid compounds as acetylcholinesterase inhibitor for the treatment of alzheimer’s disease | Authors: | Ulus, R. Esirden, İ. Aday, B. Turgut, Gurbet Çelik Şen, A. Kaya, M. |
Keywords: | Acridine Anticholinesterase activity Sulfonamide Tacrine 10 (4 bromophenyl) 3,3,6,6 tetramethyl 9 (4 nitrophenyl) 3,4,6,7,9,10 hexahydro acridine 1,8(2h,5h) dione 10 (4 chlorophenyl) 3,3,6,6 tetramethyl 9 (4 nitrophenyl) 3,4,6,7,9,10 hexahydro acridine 1,8(2h,5h) dione 4 bromo n [4 [10 (4 bromophenyl) 3,3,6,6 tetramethyl 1,8 dioxo 1,2,3,4,5,6,7,8,9,10 decahydro acridin 9 yl]phenyl]benzenesulfonamide 4 bromo n [4 [10 (4 chlorophenyl) 3,3,6,6 tetramethyl 1,8 dioxo 1,2,3,4,5,6,7,8,9,10 decahydro acridin 9 yl]phenyl]benzenesulfonamide 9 (4 aminophenyl) 10 (4 bromophenyl) 3,3,6,6 tetramethyl 3,4,6,7,9,10 hexahydro acridine 1,8(2h,5h) dione 9 (4 aminophenyl) 10 (4 chlorophenyl) 3,3,6,6 tetramethyl 3,4,6,7,9,10 hexahydro acridine 1,8(2h,5h) dione acetylcholinesterase acridine derivative cholinesterase inhibitor n [4 [10 (4 bromophenyl) 3,3,6,6 tetramethyl 1,8 dioxo 1,2,3,4,5,6,7,8,9,10 decahydro acridin 9 yl]phenyl] 2,4,6 trimethylbenzenesulfonamide n [4 [10 (4 bromophenyl) 3,3,6,6 tetramethyl 1,8 dioxo 1,2,3,4,5,6,7,8,9,10 decahydro acridin 9 yl]phenyl]benzenesulfonamide n [4 [10 (4 bromophenyl) 3,3,6,6 tetramethyl 1,8 dioxo 1,2,3,4,5,6,7,8,9,10 decahydro acridin 9 yl]phenyl]naphthalene 2 sulfonamide n [4 [10 (4 chlorophenyl) 3,3,6,6 tetramethyl 1,8 dioxo 1,2,3,4,5,6,7,8,9,10 decahydro acridin 9 yl]phenyl] 2,4,6 trimethylbenzenesulfonamide n [4 [10 (4 chlorophenyl) 3,3,6,6 tetramethyl 1,8 dioxo 1,2,3,4,5,6,7,8,9,10 decahydro acridin 9 yl]phenyl] 4 methoxybenzenesulfonamide n [4 [10 (4 chlorophenyl) 3,3,6,6 tetramethyl 1,8 dioxo 1,2,3,4,5,6,7,8,9,10 decahydro acridin 9 yl]phenyl] 4 methylbenzenesulfonamide n [4 [10 (4 chlorophenyl) 3,3,6,6 tetramethyl 1,8 dioxo 1,2,3,4,5,6,7,8,9,10 decahydro acridin 9 yl]phenyl]benzenesulfonamide sulfonamide tacrine unclassified drug Alzheimer disease Article carbon nuclear magnetic resonance cholinesterase inhibition controlled study drug synthesis enzyme activity human human cell IC50 in vitro study infrared spectroscopy mass spectrometry proton nuclear magnetic resonance SH-SY5Y cell line |
Publisher: | Birkhauser Boston | Abstract: | In this study we report that amino acridine intermediates 7 and 8 were obtained from the reduction of nitro acridine derivatives 5 and 6 that were synthesized via the condensation of dimedone, p-nitrobenzaldehyde with various amine derivatives, respectively. Then acridine sulfonamide hybrid compounds (9–18) were synthesized by the reaction of amino acridine 7, 8 with sulfonyl chlorides. The new hybrid compounds were characterized by FT-IR, 1H-NMR, 13C-NMR, and HRMS analyzes. The evaluation of in vitro anticholinesterase action of the synthesized compounds against AChE showed that some of them are potent inhibitors. Among them, compound 17 showed the most potent activity against AChE with an IC50 of 0.14 µM. © 2017, Springer Science+Business Media, LLC. | URI: | https://hdl.handle.net/11499/10852 https://doi.org/10.1007/s00044-017-2088-2 |
ISSN: | 1054-2523 |
| Appears in Collections: | Scopus İndeksli Yayınlar Koleksiyonu / Scopus Indexed Publications Collection Uygulamalı Bilimler Yüksekokulu Koleksiyonu WoS İndeksli Yayınlar Koleksiyonu / WoS Indexed Publications Collection |
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