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

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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.

About the authors

S. Yu. Maklakova

Lomonosov Moscow State University

Email: maklakovasu@yandex.ru

M. P Mazhuga

Lomonosov Moscow State University

Email: maklakovasu@yandex.ru

A. V Lopukhov

Lomonosov Moscow State University

Email: maklakovasu@yandex.ru

K. R Gibadullina

Lomonosov Moscow State University

Email: maklakovasu@yandex.ru

N. L Klyachko

Lomonosov Moscow State University

Email: maklakovasu@yandex.ru

A. G Majouga

Lomonosov Moscow State University;Dmitry Mendeleev University of Chemical Technology of Russia

Email: maklakovasu@yandex.ru

E. K Beloglazkina

Lomonosov Moscow State University

Email: maklakovasu@yandex.ru

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