Lipoic acid analogs with enhanced pharmacological activity

…, RA Casale, A Baguisi, R Beeuwkes

Index: Kates, Steven A.; Casale, Ralph A.; Baguisi, Alexander; Beeuwkes III, Reinier Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 1 p. 505 - 512

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Citation Number: 10

Abstract

Abstract Lipoic acid (1, 2-dithiolane-3-pentanoic acid) is a pharmacophore with unique antioxidant and cytoprotective properties. We synthesized a library based upon the condensation of natural and unnatural amino acids with the carboxylic acid moiety of lipoic acid. SAR studies were conducted using a cardiac ischemia-reperfusion animal model. Cytoprotective efficacy was associated with the R-enantiomer of the dithiolane. Potency of ...