Journal
ARCHIV DER PHARMAZIE
Volume 354, Issue 5, Pages -Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.202000467
Keywords
Alzheimer's disease; amyloid beta; antioxidant; cholinesterase; MAO-B; urolithins
Ask authors/readers for more resources
A series of urolithin amide derivatives were synthesized and evaluated for their inhibitory potential on cholinesterases and MAO-B. The most potent inhibitors were identified, and docking studies revealed their binding modes with the targets. These compounds showed potential for multitarget ligand design in Alzheimer's disease drug development.
A series of urolithin amide (i.e., URO-4-URO-10 and THU-4-THU-10) derivatives was designed and synthesized, and their chemical structures were confirmed with spectroscopic techniques and elemental analysis. The title compounds and synthesis intermediates (THU-1-THU-10 and URO-1-URO-10) were evaluated for their potential to inhibit acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), and monoamine oxidase B (MAO-B). Compounds THU-4 and THU-8 were found to be the most potent inhibitors for the cholinesterases and MAO-B, respectively. The docking studies were also employed to evaluate the binding modes of the most active compounds with AChE, BuChE, and MAO-B. Furthermore, the moderate-to-strong activities of the compounds were also displayed in amyloid-beta inhibition and antioxidant assay systems. The results pointed out that the urolithin scaffold can be employed in drug design studies for the development of multitarget ligands acting on various cascades shown to be important within the pathophysiology of Alzheimer's disease.
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