Publication date: February 2021
Source: Drug Discovery Today, Volume 26, Issue 2
Author(s): Sonali S. Bharate
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21 Nov 21:12
Recent developments in pharmaceutical salts: FDA approvals from 2015 to 2019
Tim Tsui likes this
02 Nov 13:47
[ASAP] Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88L265P Mutant Diffuse Large B Cell Lymphoma
by Se´bastien L. Degorce*†, Rana Anjum‡, Andrew Bloecher‡, Rodrigo J. Carbajo†, Keith S. Dillman‡, Lisa Drew‡, Christopher T. Halsall†, Eva M. Lenz†, Nicola A. Lindsay†, Michele F. Mayo‡, Jennifer H. Pink†, Graeme R. Robb†, Alan Rosen‡, James S. Scott†, and Yafeng Xue§
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01346
11 Mar 02:19
Discovery of New Monocarbonyl Ligustrazine–Curcumin Hybrids for Intervention of Drug-Sensitive and Drug-Resistant Lung Cancer
by Yong Ai, Bin Zhu, Caiping Ren, Fenghua Kang, Jinlong Li, Zhangjian Huang, Yisheng Lai, Sixun Peng, Ke Ding, Jide Tian and Yihua Zhang
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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