Discovery of novel synthetic hydroxyanisole derivatives as promising myeloperoxidase inhibitors (MPOIs) targeting atherosclerotic CVD.

Discovery of novel synthetic hydroxyanisole derivatives as promising myeloperoxidase inhibitors (MPOIs) targeting atherosclerotic CVD. ChemMedChem. 2020 May 05;: Authors: Jayaraj P, Parthasarathy S, Rajagopalan S, Aluganti C, Rajagopal D Abstract Myeloperoxidase (MPO) is known to cause oxidative stress and inflammation leading to CVD complications. MPO mediated oxidation of lipoproteins leads to dysfunctional entities altering the landscape of lipoproteins functionality. The specificity of anisole derivatives toward preventing MPO mediated oxidation to limit its harmful effects is unknown. Diligent in silico studies were accomplished for a portfolio of compounds keeping hydroxyanisole as a building block. Validation of compounds activity toward MPO inhibition is also established. The role of these chemical entities on controlling MPO-mediated oxidation of lipoproteins (LDL and HDL) is shown to agree with our approach of developing powerful MPO inhibitors. The mechanism of MPO inhibition is demonstrated to be reversible in nature. The outcome of this study reveals that there is a great opportunity available for hydroxyanisole derivatives as potential therapeutics for CVD by modulating lipid profiles, reducing atherosclerotic plaque burden and subsequently optimizing cardiovascular functions. PMID: 32368837 [PubMed - as supplied by publisher]
Source: ChemMedChem - Category: Chemistry Authors: Tags: ChemMedChem Source Type: research