Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 9, Pages 4309-4321Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm300106z
Keywords
-
Categories
Funding
- DAAD
- National Science Foundation of China (NSFC) [30973608]
- National Natural Science Foundation of China [81070967]
- Natural Science Foundation of Jiangsu Province of China [BK2009296]
Ask authors/readers for more resources
In search of multifunctional cholinesterase inhibitors as potential anti-Alzheimer drug candidates, tacrine-ferulic acid-NO donor trihybrids were synthesized and tested for their cholinesterase inhibitory activities, release of nitric oxide, vasodilator properties, cognition improving potency, and hepatotoxicity. All of the novel target compounds show higher in vitro cholinesterase inhibitory activity than tacrine. Three selected compounds (3a, 3f, and 3k) produce moderate vasorelaxation in vitro, which correlates with the release of nitric oxide. Compared to its non-nitrate dihybrid analogue (3u), the trihybrid 3f exhibits better performance in improving the scopolamine-induced cognition impairment (mice) and, furthermore, less hepatotoxicity than tacrine.
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