Pachon-Angona_2019_J.Enzyme.Inhib.Med.Chem_34_479

We describe herein the design, multicomponent synthesis and biological studies of new donepezil + chromone + melatonin hybrids as potential agents for Alzheimer's disease (AD) therapy. We have identified compound 14n as promising multitarget small molecule showing strong BuChE inhibition (IC50 = 11.90 +/- 0.05 nM), moderate hAChE (IC50 = 1.73 +/- 0.34 muM), hMAO A (IC50 = 2.78 +/- 0.12 muM), and MAO B (IC50 = 21.29 +/- 3.85 muM) inhibition, while keeping a strong antioxidant power (3.04 TE, ORAC test). Consequently, the results reported here support the development of new multitarget Donepezil + Chromone + Melatonin hybrids, such as compound 14n, as a potential drug for AD patients cure.