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Strategies in the Design of Prodrugs of Anti-HIV Agents

[ Vol. 3 , Issue. 13 ]


Theodora Calogeropoulou, Anastasia Detsi, Eleni Lekkas and Maria Koufaki   Pages 1467 - 1495 ( 29 )


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.


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


National Hellenic Research Foundation, Institute of Organic and Pharmaceutical Chemistry, 48 Vass.Constantinou Avenue, 11635 Athens, Greece.

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