期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 22, 期 1, 页码 505-512出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.10.057
关键词
Lipoic acid; Ischemia-reperfusion; SAR studies; Polymerization; Amino acids
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 library compounds was dictated by the acidic strength of the adduct. alpha-N-[(R)1,2-dithiolane-3-pentanoyl]-L-glutamyl-L-alanine, designated CMX-2043, was chosen for further pharmacologic evaluation. (C) 2013 The Authors. Published by Elsevier Ltd. All rights reserved.
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