2924-66-5Relevant 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.
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
Novel synthesis of the aldose reductase inhibitor sorbinil via amidoalkylation, intramolecular oxazolidin-5-one alkylation, and chymotrypsin resolution
Dirlam,Moore,Urban
, p. 3587 - 3591 (2007/10/02)
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