Synthesis, properties, and Anti-HIV activity of new lipophilic 3′-azido-3′-deoxythymidine conjugates containing functional phosphoric linkages

Abstract

One of the approaches to enhance the bioavailability of nucleoside reverse transcriptase HIV inhibitors is the design of their prodrugs based on 1,3-diacylglycerols, which may simulate metabolic pathways of natural lipids, thus supporting the efficacy of drug delivery to the target cells. Glycerolipid AZT conjugates with different functional phosphoric centers were synthesized by the H-phosphonate technique. Stability of the prepared prodrugs against chemical and enzymatic hydrolysis (in buffer solutions and in the presence of pancreatic lipase), as well as their anti-HIV activity against the HIV-1899A strain in human Tlymphoid MT-4 cells, were studied.

DOI: 10.1134/S1068162013020118

Extracted Key Phrases

2 Figures and Tables

Cite this paper

@article{Shastina2013SynthesisPA, title={Synthesis, properties, and Anti-HIV activity of new lipophilic 3′-azido-3′-deoxythymidine conjugates containing functional phosphoric linkages}, author={N. S. Shastina and Tatiana Maltseva and L. N. D’yakova and O. A. Lobach and M. S. Chataeva and Dmitry N Nosik and Vitaliy I Shvetz}, journal={Russian Journal of Bioorganic Chemistry}, year={2013}, volume={39}, pages={161-169} }