1053173-79-7Relevant academic research and scientific papers
Discovery, Synthesis and Evaluation of Novel Cholesterol Absorption Inhibitors
Zhu, Xiaoyun,Ji, Jianfeng,Huang, Dandan,Zhu, Yan,Tang, Chunlei,Yang, Xuan,Qian, Hai,Huang, Wenlong
experimental part, p. 426 - 433 (2012/10/07)
Chemical-based common feature pharmacophore modelling of Niemann Pick C1 Like 1 inhibitors was performed to provide some insights on the important pharmacophore features essential for Niemann Pick C1 Like 1 inhibition using Discovery Studio V2.5. After in-house database screening, a new series of substituted oxazolidinones, selected from the top ranked hits, have been synthesized and evaluated as novel cholesterol absorption inhibitors. All compounds demonstrated effect of different degrees in lowering the total cholesterol in serum, especially compounds 1a, 2a and 2d, the potency of which was comparable to that of ezetimibe. It was also found that 1a, 1d and 2d could raise high-density lipoprotein cholesterol levels markedly. Interestingly, compounds 2a-2f appeared to have the moderate potential to lower triglyceride levels, which were superior to that of normal cholesterol absorption inhibitors including ezetimibe. Two classes of novel substituted oxazolidinones were identified by virtual screening as the candidates of cholesterol absorption inhibitors to treat coronary artery disease. All compounds demonstrated effect of different degrees in lowering the total cholesterol in serum. Interestingly, compounds 2a-2f appeared to have the moderate potential to lower triglyceride levels, which were superior to that of normal cholesterol absorption inhibitors including ezetimibe.
Substituted oxazolidinones as novel NPC1L1 ligands for the inhibition of cholesterol absorption
Pfefferkorn, Jeffrey A.,Larsen, Scott D.,Huis, Chad Van,Sorenson, Roderick,Barton, Tom,Winters, Thomas,Auerbach, Bruce,Wu, Chenyan,Wolfram, Thaddeus J.,Cai, Hongliang,Welch, Kathleen,Esmaiel, Nadia,Davis, JoAnn,Bousley, Richard,Olsen, Karl,Mueller, Sandra Bak,Mertz, Thomas
, p. 546 - 553 (2008/09/19)
Cholesterol absorption inhibition (CAI) represents an important treatment option for hypercholesterolemia. Herein, we report the design and evaluation of a series of substituted oxazolidinones as ligands for the Niemann Pick C1 Like 1 (NPC1L1) protein, a
OXAZOLIDINONES AS CHOLESTEROL ABSORPTION INHIBITORS
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Page/Page column 64, (2008/12/07)
Novel oxazolidinones and pharmaceutical compositions are described, as are methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholeserolemia, and atherosclerosis.
