Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 22, Pages 6649-6652Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.09.013
Keywords
Berberine derivatives; Dual inhibitors; Acetylcholinesterase; Butyrylcholinesterase; Molecular modeling
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Funding
- Natural Science Foundation of China [20972198]
- Ministry of Science and Technology of China [2009ZX09501-017]
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Berberine derivatives with substituted amino groups linked at the 9-position using different carbon spacers were designed, synthesized, and biologically evaluated as inhibitors of acetylcholinesterase. Compound 10b, with a cyclohexylamino group linked to berberine by a three carbon spacer, gave the most potent inhibitor activity with an IC50 of 0.020 mu M for AChE. Kinetic studies revealed mixed inhibition of AChE, and molecular modeling simulations of the AChE-inhibitor complex confirmed that compounds bound to both the catalytic active site and the peripheral anionic site. (C) 2010 Elsevier Ltd. All rights reserved.
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