| Literature DB >> 33571811 |
Pritam Thapa1, Sunil P Upadhyay2, William Z Suo3, Vikas Singh4, Prajwal Gurung5, Eung Seok Lee6, Ram Sharma2, Mukut Sharma2.
Abstract
Chalcone [(E)-1,3-diphenyl-2-propene-1-one], a small molecule with α, β unsaturated carbonyl group is a precursor or component of many natural flavonoids and isoflavonoids. It is one of the privileged structures in medicinal chemistry. It possesses a wide range of biological activities encouraging many medicinal chemists to study this scaffold for its usefulness to oncology, infectious diseases, virology and neurodegenerative diseases including Alzheimer's disease (AD). Small molecular size, convenient and cost-effective synthesis, and flexibility for modifications to modulate lipophilicity suitable for blood brain barrier (BBB) permeability make chalcones a preferred candidate for their therapeutic and diagnostic potential in AD. This review summarizes and highlights the importance of chalcone and its analogs as single target small therapeutic agents, multi-target directed ligands (MTDLs) as well as molecular imaging agents for AD. The information summarized here will guide many medicinal chemist and researchers involved in drug discovery to consider chalcone as a potential scaffold for the development of anti-AD agents including theranostics. Published by Elsevier Inc.Entities:
Keywords: Alzheimer’s disease; Amyloid beta inhibition; Chalcone; Cholinesterase inhibitors; Molecular probes; Multi-target directed ligands; Neuroinflammation; Theranostic
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Year: 2021 PMID： 33571811 PMCID： PMC7928223 DOI： 10.1016/j.bioorg.2021.104681
Source DB: PubMed Journal: Bioorg Chem ISSN： 0045-2068 Impact factor: 5.307