Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.5c00182
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07 Aug 16:19
[ASAP] A Medicinal Chemistry Perspective on Lactate Dehydrogenase: Current Status and Future Directions
by Wanyi Pan, Chengpeng Tao, Yi Wu, and Feng Jiang
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Recent developments in pharmaceutical salts: FDA approvals from 2015 to 2019
Publication date: February 2021
Source: Drug Discovery Today, Volume 26, Issue 2
Author(s): Sonali S. Bharate
Tim Tsui likes this
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[ASAP] Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88L265P Mutant Diffuse Large B Cell Lymphoma
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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01346
11 Mar 02:19
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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.5b01203
20 Apr 08:00
Lipoic acid analogs with enhanced pharmacological activity
Publication date: 1 January 2014
Source:Bioorganic & Medicinal Chemistry, Volume 22, Issue 1
Author(s): Steven A. Kates , Ralph A. Casale , Alexander Baguisi , Reinier Beeuwkes III
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.
Source:Bioorganic & Medicinal Chemistry, Volume 22, Issue 1
Author(s): Steven A. Kates , Ralph A. Casale , Alexander Baguisi , Reinier Beeuwkes III
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.
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