| Title : Discovery of XEN445: A potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice - Sun_2013_Bioorg.Med.Chem_21_7724 |
| Author(s) : Sun S , Dean R , Jia Q , Zenova A , Zhong J , Grayson C , Xie C , Lindgren A , Samra P , Sojo L , van Heek M , Lin L , Percival D , Fu JM , Winther MD , Zhang Z |
| Ref : Bioorganic & Medicinal Chemistry , 21 :7724 , 2013 |
|
Abstract :
Endothelial lipase (EL) activity has been implicated in HDL metabolism and in atherosclerotic plaque development; inhibitors are proposed to be efficacious in the treatment of dyslipidemia related cardiovascular disease. We describe here the discovery of a novel class of anthranilic acids EL inhibitors. XEN445 (compound 13) was identified as a potent and selective EL inhibitor, that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice. |
| PubMedSearch : Sun_2013_Bioorg.Med.Chem_21_7724 |
| PubMedID: 24211162 |
| Gene_locus related to this paper: human-LIPG |
| Inhibitor | XEN445 |
| Gene_locus | human-LIPG |
Sun S, Dean R, Jia Q, Zenova A, Zhong J, Grayson C, Xie C, Lindgren A, Samra P, Sojo L, van Heek M, Lin L, Percival D, Fu JM, Winther MD, Zhang Z (2013)
Discovery of XEN445: A potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice
Bioorganic & Medicinal Chemistry
21 :7724
Sun S, Dean R, Jia Q, Zenova A, Zhong J, Grayson C, Xie C, Lindgren A, Samra P, Sojo L, van Heek M, Lin L, Percival D, Fu JM, Winther MD, Zhang Z (2013)
Bioorganic & Medicinal Chemistry
21 :7724