Synthesis and inhibitory activity of atorvastatin conjugate with a branched asialoglycoprotein receptor ligand with 3 N-acetyl-d-galactosamine residues
Svetlana Yu. Maklakova, Maria P. Mazhuga, Anton V. Lopukhov, Karina R. Gibadullina, Natalia L. Klyachko, Alexander G. Majouga, Elena Kimovna Beloglazkina · Журнал органической химии · 2023
The novel atorvastatin conjugate was synthesized in a multi-step procedure using branched N -acetylgalactosamine ligand for asialoglycoprotein receptor targeting. The molar solubility of the obtained conjugate was 6.1±0.9 mM, which is almost 60 times higher than that of unmodified atorvastatin. The hydrolysis products of the conjugate demonstrated effective inhibition of 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase.