Synthesis of propynyloxy substituted some novel aurones as potent Cathepsin B inhibitors (original) (raw)

Chemical Data Collections, 2020

Abstract

Abstract A two-step synthesis was designed to develop a novel series of 6-propynyloxyaurones, 2(a-r). The synthesized aurone derivatives were characterized by their IR, NMR, and mass spectrometry data. The present study proposes these aurones as anti-inflammatory and anti-Alzheimer candidates on the basis of their cathepsin B inhibitory activities. Anti-cathepsin activity of some of the synthesized aurones was found, either equivalent to or higher than the reference drugs, aspirin and curcumin at submicromolar concentrations. Among the studied compounds, 2e, 2i, 2n, 2q, and 2r exhibited much higher activity in comparison to the standard drugs. The molecular docking study also highlighted compound 2r for its greater anti-cathepsin B activity among all the designed aurones.

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