![]() ![]() ![]() ![]() It also shows interesting results when it comes to a pharmacophore study based on ezetimibe as the main ligand in lowering blood cholesterol levels, revealing which substituents on the azetidine-2-one ring are more similar to the ezetimibe skeleton and will more likely bind to NPC1L1 than ezetimibe.Ĭholesterol is an essential structural component of mammalian cell membranes and is the precursor of vitamin D, bile salts and steroid hormones a high level of this substance in an organism can be dangerous. ![]() A subsequent inversion of ester and acid functionality paves the way to the lactam core after monodebenzylation and lactam formation. The route involves a domino process: allylic acetate rearrangement, stereoselective Ireland–Claisen rearrangement and asymmetric Michael addition, which provides a δ-amino acid derivative with full stereochemical control. A convenient asymmetric synthesis of (2 S,3 S)- N-α-( R)-methylbenzyl-3-methoxycarbonylethyl-4-methoxyphenyl β-lactam is described starting from Baylis–Hillman adducts. A ligand-based study on ezetimibe analogues is reported, together with one-hit synthesis, highlighted in the study. Ezetimibe is a well-known drug that lowers blood cholesterol levels by reducing its absorption in the small intestine when joining to Niemann-Pick C1-like protein (NPC1L1). ![]()
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