Diaminoindanes as microsomal triglyceride transfer protein inhibitors

…, M Jeune, R Steele, J Wasvery, Z Stephan…

文献索引：Ksander; DeJesus; Yuan; Fink; Moskal; Carlson; Kukkola; Bilci; Wallace; Neubert; Feldman; Mogelesky; Poirier; Jeune; Steele; Wasvery; Stephan; Cahill; Webb; Navarrete; Lee; Gibson; Alexander; Sharif; Hospattankar Journal of Medicinal Chemistry, 2001 , vol. 44, # 26 p. 4677 - 4687

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被引用次数: 41

摘要

The synthesis and biological activities of biarylamide-substituted diaminoindanes as microsomal triglyceride transfer protein (MTP) inhibitors are described. One of the more potent compounds, 8aR, inhibited both the secretion of apoB from Hep G2 cells and the MTP- mediated transfer of triglycerides between synthetic acceptor and donor liposomes with IC50 values of 0.7 and 70 nM, respectively. In normolipidemic rats and dogs, oral administration ...