Synthesis and inhibitory activity of atorvastatin conjugate with a branched asialoglycoprotein receptor ligand with 3 <i>N</i>-acetyl-d-galactosamine residues-Reference-Cited by-同舟云学术

Synthesis and inhibitory activity of atorvastatin conjugate with a branched asialoglycoprotein receptor ligand with 3 <i>N</i>-acetyl-d-galactosamine residues

Published:2023-02-15 Issue:2 Volume:59 Page:217-227
ISSN:0514-7492
Container-title:Журнал органической химии
language:
Short-container-title:Žurnal organičeskoj himii

Author:

Maklakova S. Yu.¹,Mazhuga M. P¹,Lopukhov A. V¹,Gibadullina K. R¹,Klyachko N. L¹,Majouga A. G¹²,Beloglazkina E. K¹

Affiliation:

1. Lomonosov Moscow State University

2. Dmitry Mendeleev University of Chemical Technology of Russia

Abstract

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.

Publisher

The Russian Academy of Sciences

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