Chromone Scaffolds in the Treatment of Alzheimer's and Parkinson's Disease: An Overview

Abstract

Neurodegenerative disorders such as Alzheimer's (AD) and Parkinson's disease (PD) usually starts gradually and progressively worsens, and are recognized as one of the leading causes of mortality and disability worldwide. Presently, all the available drugs for AD and PD are only for symptomatic relief, and are not capable of preventing and curing the disease. Chromone is a privileged structure for designing of novel drug agents with pharmacological potential, specifically in the field of AD and PD. The present review is focused on the significance of chromones as novel drug agents for the treatment of AD and PD. Chromone based acetylcholinesterase, butyrylcholinesterase, monoamine oxidase B, β-Secretase-1, inhibitors are discussed. As AD belongs to one of the most complex and multifactorial disorders, therefore, the multi-target drugs are urgently required. However, there has been a substantial research effort in designing multi-target drug agents. Therefore, in this review, chromone based multi-target inhibitors are also discussed. Furthermore, future directions for designing and developing potent chromone based drugs are reported.

Development of new Alzheimer's disease drug candidates using donepezil as a key model

“…Chromone (1-benzopyran-4-one) exhibited AChE, BChE, MAO-B, and β-secretase inhibitory activity. [61] Melatonin showed antioxidant activity as we illustrated previously. Therefore, designing a hybridized model combining chromone, melatonin, and DNP scaffolds could give promising multitarget anti-Alzheimer agents.…”

The Chemotype of Chromanones as a Privileged Scaffold for Multineurotarget Anti-Alzheimer Agents

“…Chromenones have been extensively investigated as MSMs. 7,26,27,34,36 Despite the obvious similarity of both chemotypes, the structural features diverge due to the aromatic character of the γ-pyrone ring in chromenones which was confirmed by nucleus independent chemical shift values. 50 Chromenone XXI, the direct structural counterpart of 19, exhibited weaker effects at the five targets (Figure 3).…”

“…Strong efforts in drug discovery are based on the first line AD hypotheses, tau- and beta-amyloid. Moreover, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) or monoamine oxidases (MAOs) constitute frequently selected biological targets for the development of AD therapeutics. − …”

Anti-Insect Properties of Penicillium Secondary Metabolites

“…Other compounds in Figure 2 belong to different classes, also representing models for insights into the structural properties of AChE-inhibitors. This is the case for anthraquinones, such as aloe-emodin and citrorosein [ 137 ], xanthones (e.g., pinseline) [ 138 ], and chromones (e.g., maritimin and analogues) [ 139 ].…”