Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 12, Issue 5, Pages 801-814Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c3ob42010h
Keywords
-
Categories
Funding
- Innovative Research Team in University [IRT1193]
- Priority Academic Program Development of Jiangsu Higher Education Institutions (PAPD), Project of Graduate Education Innovation of Jiangsu Province [CXZZ13_0320]
Ask authors/readers for more resources
A series of tacrine-rhein hybrid compounds have been designed and synthesized as novel multifunctional potent ChE inhibitors. Most of the compounds inhibited ChEs in the nanomolar range in vitro effectively. Compound 10b was one of the most potent inhibitors and was 5-fold more active than tacrine toward AChE, and it also showed a moderate BuChE inhibition with an IC50 value of 200 nM. Kinetic and molecular modeling studies of 10b also indicated that it was a mixed-type inhibitor binding simultaneously to the active and peripheral sites of AChE. In inhibition of the AChE-induced A beta aggregation assay, compound 10b (70.2% at 100 mu M) showed the greatest inhibitory activity. In addition, 10b showed metal-chelating property and low hepatotoxicity. These results suggested that 10b might be an excellent multifunctional agent for AD treatment.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available