Chalcone containing hydroxyl- and amino-group, a privileged scaffold in drug discovery: Developing in anti-Alzheimer’s and anti-Parkinson’s properties

Chalcones have multiple targets and multifaceted pharmacological properties. Besides, chalcone structures possess the advantages, such as small molecular weight, convenient synthesis method, lower cost efficiency, and possibility for further structural modification by changing physical and chemical properties. Therefore, in the drug discovery process, chalcone scaffolds are considered to be one of the most preferred frameworks. Among neurodegenerative conditions, Alzheimer’s disease (AD) and Parkinson’s disease (PD) are widely prevalent, with age being the biggest risk factor. In addition, many reports have evidenced that hydroxyl groups or amine groups could become other functional groups, containing ethers, esters, and amides, etc., in which the introduction of the hydroxyl or amino groups on chalcone frameworks, instead of ethers, esters, or amides, could enhance monoamine oxidases (MAOs), ChEs, beta-site amyloid precursor protein cleaving enzyme1 (BACE1), or β-amyloid (Aβ) inhibitory activities. So, the development of chalcone compounds having hydroxyl or amino groups for AD and PD therapy is one of the most interesting research topics. As a result, this article aims to highlight the latest progress of chalcone-containing hydroxyl or amine substitution related to pharmacophores as selective MAO, ChE, or BACE1 inhibitors for AD and PD prophylaxis in medicinal chemistry development processes for AD and PD.