Heterocyclic ring scaffolds as small-molecule cholesterol absorption inhibitors
- 24 August 2005
- journal article
- research article
- Published by Royal Society of Chemistry (RSC) in Organic & Biomolecular Chemistry
- Vol. 3 (19) , 3514-3523
- https://doi.org/10.1039/b510100j
Abstract
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.Keywords
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