Strategies in the Design of Prodrugs of Anti-HIV Agents

Author(s): Theodora Calogeropoulou, Anastasia Detsi, Eleni Lekkas, Maria Koufaki

Journal Name: Current Topics in Medicinal Chemistry

Volume 3 , Issue 13 , 2003

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Control of AIDS requires development of special therapeutic strategies in order to reduce the level of monocyte / macrophage HIV infection, to prevent spread of HIV within the monocyte / macrophage reservoir, to maintain a therapeutically effective drug concentration in sanctuaries such as the brain and to overcome the problem of cellular resistance mechanisms. A popular approach towards this end has been the development of prodrugs of anti-HIV drugs. This review covers the different strategies devised for the design of prodrugs of anti-HIV agents with emphasis on the recent findings in this field of research. Thus, prodrugs of nucleoside reverse transcriptase inhibitors (NRTIs) including, 5-O carboxylic ester derivatives, 5-O- monophosphate analogues, macromolecular derivatives, prodrugs of purine nucleosides, prodrugs of acyclic nucleosides, homo and hetero dinucleotides, prodrugs of non-classical nucleoside analogues, boranophosphate triesters of NRTIs, and prodrugs of protease inhibitors including acyl-substituted prodrugs, prodrugs with increased water solubility, monophosphate prodrugs, and conjugates of HIV protease inhibitors with a reverse transcriptase inhibitor through spontaneously cleavable linkers, constitute the subject of this review.

Keywords: prodrug, pronucleotide, anti-hiv, conjugate, nucleoside reverse transcriptase inhibitor, protease inhibitor

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Article Details

Year: 2003
Page: [1467 - 1495]
Pages: 29
DOI: 10.2174/1568026033451763
Price: $65

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