ADA-Bypass by lipophilic cycloSal-ddAMP pro-nucleotides A second example of the efficiency of the cycloSal-Concept

The synthesis of lipophilic pro-nucleotides of ddAMP 2 based on cycloSal-ddAMP 3a-c is described. Phosphotriesters 3 released ddAMP 2 selectively by a controlled, chemically induced tandem reaction. CycloSal-phosphotriesters 3 exhibited antiviral activity against HIV-1/HIV-2 in CEM cells that where...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1997-06, Vol.7 (12), p.1577-1582
Main Authors: Meier, Chris, Knispel, Tina, De Clercq, E., Balzarini, Jan
Format: Article
Language:English
Subjects:
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Biological and medical sciences
Medical sciences
Pharmacology. Drug treatments
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Summary:The synthesis of lipophilic pro-nucleotides of ddAMP 2 based on cycloSal-ddAMP 3a-c is described. Phosphotriesters 3 released ddAMP 2 selectively by a controlled, chemically induced tandem reaction. CycloSal-phosphotriesters 3 exhibited antiviral activity against HIV-1/HIV-2 in CEM cells that where by a factor up to hundred higher as compared to ddA 1. The synthesis, hydrolysis data, HIV-1/ HIV-2 activity in CEM/O cells and the ADA stability of the new cycloSal-ddAMP pro-nucleotides 3a-c are described.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(97)00265-5