65626-22-4Relevant articles and documents
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.
HEPATITIS C VIRUS INHIBITORS
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, (2012/03/09)
The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment o
IMIDAZOPYRIDIN-2-ONE DERIVATIVES
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Page/Page column 26, (2011/04/24)
A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.
