Abstract
Pronucleotides represent a promising alternative to improve the biological activity of nucleoside analogues against different viral diseases. The basic idea is to achieve nucleotide delivery into cells, bypassing limitations with intracellular formation of nucleotides from their nucleoside precursors. The cycloSal-concept is one of several pronucleotide systems reported so far. For the nucleoside analogue d4T, the cycloSal-approach improved antiviral potency. The basic idea, chemistry, different structural modifications and their effects on the antiviral potency of the cycloSal-d4TMP triesters have been discussed in this review.
Keywords: pronucleotides-structural variations, biological activity of nucleoside analogues, enzymatically triggered pronucleotides, hplc-analyzed studies, enzymatic degradation
Current Topics in Medicinal Chemistry
Title: cycloSal-d4TMP Pronucleotides-Structural Variations, Mechanistic Insights and Antiviral Activity
Volume: 2 Issue: 10
Author(s): Chris Meier, Jurgen Renze, Christian Ducho and Jan Balzarini
Affiliation:
Keywords: pronucleotides-structural variations, biological activity of nucleoside analogues, enzymatically triggered pronucleotides, hplc-analyzed studies, enzymatic degradation
Abstract: Pronucleotides represent a promising alternative to improve the biological activity of nucleoside analogues against different viral diseases. The basic idea is to achieve nucleotide delivery into cells, bypassing limitations with intracellular formation of nucleotides from their nucleoside precursors. The cycloSal-concept is one of several pronucleotide systems reported so far. For the nucleoside analogue d4T, the cycloSal-approach improved antiviral potency. The basic idea, chemistry, different structural modifications and their effects on the antiviral potency of the cycloSal-d4TMP triesters have been discussed in this review.
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Cite this article as:
Meier Chris, Renze Jurgen, Ducho Christian and Balzarini Jan, cycloSal-d4TMP Pronucleotides-Structural Variations, Mechanistic Insights and Antiviral Activity, Current Topics in Medicinal Chemistry 2002; 2 (10) . https://dx.doi.org/10.2174/1568026023393183
DOI https://dx.doi.org/10.2174/1568026023393183 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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