6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors |
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| Authors: | Schott Yvonne Decker Michael Rommelspacher Hans Lehmann Jochen |
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| Institution: | 1. Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, The MOE Key Laboratory for Standardization of Chinese Medicines and the SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines; Shanghai R&D Centre for Standardization of Chinese Medicines, Shanghai 201203, China;2. Shanghai TCM-integrated Hospital, Shanghai University of Traditional Chinese Medicine, 230 Baoding Road, Shanghai 200082, China;3. Department of Pharmacy, Changzheng Hospital, Second Military Medical University, Shanghai 200003, China;4. Department of Pharmacy, Shanghai Jiao Tong University Affiliated Sixth People''s Hospital, Shanghai 200233, China;5. Department of Core Facility of Basic Medical Sciences, Shanghai Jiao Tong University School of Medicine, Shanghai 200025, China |
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| Abstract: | In the course of studies directed toward the discovery of novel acetyl- and butyrylcholinesterase (AChE and BChE) inhibitors for the treatment of Alzheimer's disease, we focused on beta-carbolines (BCs). 6-Oxygenated beta-carboline and beta-carbolinium derivatives based on the serotonin template were synthesized and tested in vitro for their ability to inhibit AChE and BChE, respectively. Particularly the carbolinium salts, which can be formed by intracerebral methylation out of the tertiary-BC prodrugs, show inhibitory activity levels reaching those of galantamine, physostigmine, and rivastigmine. |
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