Abstract
Hyperlipidemia is a common cardiovascular disease characterized by elevated lipid level in association with disordered lipoproteins metabolism. Atorvastatin, an HMG-CoA reductase inhibitor, has been developed as an antihyperlipidaemic agent and proved to exhibit antioxidant activity against lipid peroxidation. The two hydroxyl metabolites of atorvastatin, Ortho-hydroxy-atorvastatin and para-hydroxy-atorvastatin, are equipotent to their parent compound. Anethol trithione is a kind of liver protecting agent used to treat the hepatobiliary disease-related symptoms. Desmethyl anethol trithione, the degradation product of anethol trithione, keeps the related activity of anethol trithione and it is suitable for developing novel prodrugs. In this letter, a series of atorvastatin derivatives was designed as lipid regulators based on the structures of para-hydroxy-atorvastatin and desmethyl anethol trithione. Preliminary biological evaluation suggested compound 11a presented promising antihyperlipidemic, antioxidant activity and plasma stability.
Keywords: Hyperlipidemia, Atorvastatin derivatives, Anethol trithione, Antihyperlipidaemic activity, Antioxidant activity, Plasma stability.
Letters in Drug Design & Discovery
Title:Synthesis and Biological Evaluation of Atorvastatin Derivatives as Novel HMG-CoA Reductase Inhibitors
Volume: 10 Issue: 9
Author(s): Jiayi Tong, Naxin Wang and Hua Xiao
Affiliation:
Keywords: Hyperlipidemia, Atorvastatin derivatives, Anethol trithione, Antihyperlipidaemic activity, Antioxidant activity, Plasma stability.
Abstract: Hyperlipidemia is a common cardiovascular disease characterized by elevated lipid level in association with disordered lipoproteins metabolism. Atorvastatin, an HMG-CoA reductase inhibitor, has been developed as an antihyperlipidaemic agent and proved to exhibit antioxidant activity against lipid peroxidation. The two hydroxyl metabolites of atorvastatin, Ortho-hydroxy-atorvastatin and para-hydroxy-atorvastatin, are equipotent to their parent compound. Anethol trithione is a kind of liver protecting agent used to treat the hepatobiliary disease-related symptoms. Desmethyl anethol trithione, the degradation product of anethol trithione, keeps the related activity of anethol trithione and it is suitable for developing novel prodrugs. In this letter, a series of atorvastatin derivatives was designed as lipid regulators based on the structures of para-hydroxy-atorvastatin and desmethyl anethol trithione. Preliminary biological evaluation suggested compound 11a presented promising antihyperlipidemic, antioxidant activity and plasma stability.
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Cite this article as:
Tong Jiayi, Wang Naxin and Xiao Hua, Synthesis and Biological Evaluation of Atorvastatin Derivatives as Novel HMG-CoA Reductase Inhibitors, Letters in Drug Design & Discovery 2013; 10 (9) . https://dx.doi.org/10.2174/15701808113106660020
DOI https://dx.doi.org/10.2174/15701808113106660020 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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