488835-85-4Relevant academic research and scientific papers
NOVEL LYSOPHOSPHATIDIC ACID RECEPTOR SELECTIVE ANTAGONISTS
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Page/Page column 95-96, (2008/06/13)
The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.
Initial structure-activity relationships of lysophosphatidic acid receptor antagonists: Discovery of a high-affinity LPA1/LPA3 receptor antagonist
Heasley, Brian H.,Jarosz, Renata,Lynch, Kevin R.,Macdonald, Timothy L.
, p. 2735 - 2740 (2007/10/03)
A recently reported dual LPA1/LPA3 receptor antagonist (VPC12249, 1) has been modified herein so as to optimize potency and selectivity at LPA receptors. Compounds containing variation in the acyl lipid chain and linker region have been synthesized and screened for activity at individual LPA receptors. LPA1-selective (14b) and LPA 3-selective (10g,m) compounds of modest potency have been discovered. Additionally, 2-pyridyl derivative 10t exhibits a Ki value of 18nM at the LPA1 receptor and is significantly more potent than 1 at the LPA3 receptor. This paper describes the synthetic methods, biological evaluation, and structure-activity relationships (SARs) of LPA receptor antagonists.
Diastereoselective synthesis of all stereoisomers of β-methoxytyrosine, a component of papuamides
Okamoto, Naoki,Hara, Osamu,Makino, Kazuishi,Hamada, Yasumasa
, p. 9210 - 9215 (2007/10/03)
β-Methoxytyrosine (β-OMeTyr) is a stereoundefined component of papuamides A and B, novel cyclodepsipeptides, with anti-HIV and cytotoxic activities. For structural determination and total synthesis of papuamides, all stereoisomers of β-OMeTyr were stereos
