2924-66-5Relevant academic research and scientific papers
Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2)
Woolford, Alison J.-A.,Day, Philip J.,Bénéton, Véronique,Berdini, Valerio,Coyle, Joseph E.,Dudit, Yann,Grondin, Pascal,Huet, Pascal,Lee, Lydia Y. W.,Manas, Eric S.,McMenamin, Rachel L.,Murray, Christopher W.,Page, Lee W.,Patel, Vipulkumar K.,Potvain, Florent,Rich, Sharna J.,Sang, Yingxia,Somers, Don O.,Trottet, Lionel,Wan, Zehong,Zhang, Xiaomin
supporting information, p. 10738 - 10749 (2016/12/16)
Lp-PLA2 has been explored as a target for a number of inflammation associated diseases, including cardiovascular disease and dementia. This article describes the discovery of a new fragment derived chemotype that interacts with the active site of Lp-PLA2. The starting fragment hit was discovered through an X-ray fragment screen and showed no activity in the bioassay (IC50 > 1 mM). The fragment hit was optimized using a variety of structure-based drug design techniques, including virtual screening, fragment merging, and improvement of shape complementarity. A novel series of Lp-PLA2 inhibitors was generated with low lipophilicity and a promising pharmacokinetic profile.
Copper(ii)-catalyzed C-O coupling of aryl bromides with aliphatic diols: Synthesis of ethers, phenols, and benzo-fused cyclic ethers
Liu, Yajun,Park, Se Kyung,Xiao, Yan,Chae, Junghyun
supporting information, p. 4747 - 4753 (2014/06/24)
A highly efficient copper-catalyzed C-O cross-coupling reaction between aryl bromides and aliphatic diols has been developed employing a cheaper, more efficient, and easily removable copper(ii) catalyst. A broad range of aryl bromides were coupled with aliphatic diols of different lengths using 5 mol% CuCl2 and 3 equivalents of K2CO3 in the absence of any other ligands or solvents to afford the corresponding hydroxyalkyl aryl ethers in good to excellent yields. In this newly developed protocol, aliphatic diols have multilateral functions as coupling reactants, ligands, and solvents. The resulting hydroxyalkyl aryl ethers were further readily converted into the corresponding phenols, presenting a valuable alternative way to phenols from aryl bromides. Furthermore, it was demonstrated that they are useful intermediates for more advanced molecules such as benzofurans and benzo-fused cyclic ethers. This journal is
OXYCARBAMOYL COMPOUNDS AND THE USE THEREOF
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, (2010/01/07)
The invention relates to oxycarbamoyl compounds of Formula I: The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockadeof calcium channels, and particularly N-type calcium channe
SPHINGOSINE-1 -PHOSPHATE RECEPTOR AGONIST AND ANTAGONIST COMPOUNDS
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Page/Page column 122-123, (2008/12/07)
The present invention is directed to novel, potent, and selective agents, which are agonists or antagonists of the one or more of the individual receptors of the S1P receptor family. The compounds of the invention are useful as therapeutics for treating medical conditions associated with agonism or antagonism of the individual receptors of the S1P receptor family.
Method of treating lipidemia with aryloxyalkylaminobenzoic acids and esters
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, (2008/06/13)
Aryloxyalkylaminobenzoic acids and esters as hypolipemic compounds.
