Background:
Alzheimer's disease (AD) is an irreversible and progressive neurodegeneration, with a multifactorial pathophysiology, including cholinergic deficit, amyloid plaques, neurofibrillary tangles, oxidative stress, and neurodegeneration. Despite the severity of the disease, the therapeutic arsenal is limited, arousing the interest of researchers to search
for substances that can act on these markers.
Objective:
In this review, we highlight some relevant points: the ability of chalcones to act on different targets related to the
pathophysiology of Alzheimer's disease: cholinesterases, amyloid peptide, beta-secretase and other biomarkers.
Method:
This mini-review covered the literature concerning chalcones bioactivity from 2010 until now. In addition to the
theoretical review, we included the prediction of physicochemical properties, using SwissADME software.
Results:
We found that the majority of the chalcones have been tested against cholinesterases, with moderate to good potencies, but in recent years, the number of publications related to targets of the amyloid hypothesis has been growing. Regarding the physicochemical properties, chalcones have a good profile, except the water solubility, which is not favorable.
Conclusion:
The most important characteristic of these molecules,is the given that many of the examples mentioned here
act on more than one target, characterizing them as multi-target compounds. Regarding predicted properties, solubility
stands out as the most problematic one, however these structures can incorporate functional groups that circumvent this
problem of solubility without interfering in the biological activity.
P2-008: A curcumin analogue as a “smart” fluorescent probe with potential capacity for in vivo
imaging the full course of amyloidosis of Alzheimer's disease
