795306-87-5Relevant academic research and scientific papers
Heterocyclic ring scaffolds as small-molecule cholesterol absorption inhibitors
Ritter, Tobias,Kvaerno, Lisbet,Werder, Moritz,Hauser, Helmut,Carreira, Erick M.
, p. 3514 - 3523 (2007/10/03)
Enantio- and diastereoselective syntheses of a substituted oxazolidinone, isoxazoline and pyrazoline as β-lactam surrogates are described. The substituted heterocycles were designed to incorporate side chains closely resembling those found in the β-lactam cholesterol absorption inhibitor ezetimibe (1). Additionally, the in vitro inhibitory efficacy of the novel compounds as cholesterol absorption inhibitors is reported using a brush border membrane vesicle assay. The Royal Society of Chemistry 2005.
An in vitro assay for evaluation of small-molecule inhibitors of cholesterol absorption
Kvaerno, Lisbet,Ritter, Tobias,Werder, Moritz,Hauser, Helmut,Carreira, Erick M.
, p. 4653 - 4656 (2007/10/03)
Giving cholesterol the brush off: An intestinal brush border membrane vesicle assay has been devised for the convenient in vitro testing of small molecules for inhibition of cholesterol absorption. The assay was used to identify new nonhydrolyzable glycosides as potent cholesterol-absorption inhibitors and an oxazolidinone as an effective replacement of the β-lactam scaffold of ezetimibe (1).
