Document Detail


Lipoic acid analogs with enhanced pharmacological activity.
MedLine Citation:
PMID:  24316353     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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. α-N-[(R)-1,2-dithiolane-3-pentanoyl]-l-glutamyl-l-alanine, designated CMX-2043, was chosen for further pharmacologic evaluation.
Authors:
Steven A Kates; Ralph A Casale; Alexander Baguisi; Reinier Beeuwkes
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-11-14
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  -     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2013 Nov 
Date Detail:
Created Date:  2013-12-9     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2013 The Authors. Published by Elsevier Ltd.. All rights reserved.
Affiliation:
Ischemix, LLC, 63 Great Road, Maynard, MA 01759, United States. Electronic address: skates@ischemix.com.
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