PMID: 9525429Apr 3, 1998Paper

Marked inhibitory activity of masked aryloxy aminoacyl phosphoramidate derivatives of dideoxynucleoside analogues against visna virus infection

Journal of Acquired Immune Deficiency Syndromes and Human Retrovirology : Official Publication of the International Retrovirology Association
J BalzariniH Thormar

Abstract

Lipophilic masked aryloxyaminoacylphosphoramidate derivatives of 2',3'-dideoxynucleoside (ddN) analogues with potent anti-HIV activity (i.e., stavudine [d4T], azidothymidine [AZT], dideoxycytidine [ddC], 3'thio-2',3'-dideoxy cytidine [3TC], dideoxyadenosine [ddA], and 2',3'-didehydro-2',3'-dideoxyadenosine [d4A]) activity were evaluated for their activity against visna virus (VV) in sheep choroid plexus (SCP) cells. The activity of several prodrug derivatives against VV proved markedly superior to that of the corresponding free ddN analogues. In particular, the d4A and ddA prodrug derivatives were exquisitely inhibitory in this model system (50% effective concentration [EC50], < or = 0.003 microM), and their anti-VV potency exceeded by at least 200-fold the antiviral potency of the corresponding free nucleosides. Marked differences were noted in the anti-VV potencies of several of the test compounds depending on the nature of the amino acid linked to the 5'-phosphate moiety, the nature of the nucleoside, or both. In view of the stability of the prodrugs in lamb serum, the VV infection model in lambs may be considered highly useful for investigating the in vivo antiretroviral efficacy of these type of drugs, particularly the d4T...Continue Reading

References

Jan 1, 1991·AIDS·J P Moore, P L Nara
Apr 1, 1990·Proceedings of the National Academy of Sciences of the United States of America·H EgberinkM Koolen
Jan 1, 1989·Proceedings of the National Academy of Sciences of the United States of America·J BalzariniE De Clercq
Apr 11, 1995·Proceedings of the National Academy of Sciences of the United States of America·H ThormarE De Clercq
Jul 9, 1996·Proceedings of the National Academy of Sciences of the United States of America·J BalzariniC McGuigan

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Citations

Jan 1, 2016·BioImpacts : BI·Jaleh BararYadollah Omidi
Mar 20, 2002·Antiviral Chemistry & Chemotherapy·J BalzariniC Meier
Nov 4, 2000·Medicinal Research Reviews·C R WagnerE J McIntee

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