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5′‐Phosphonate Derivatives of 2′,3′‐Dideoxy‐3′‐Thiacytidine as New Anti‐HIV Prodrugs
Author(s) -
Khandazhinskaya Anastasia L.,
Jasko Maxim V.,
Karpenko Inna L.,
Solyev Pavel N.,
Golubeva Natalia A.,
Kukhanova Marina K.
Publication year - 2011
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2011.01129.x
Subject(s) - prodrug , phosphonate , pharmacokinetics , pharmacology , nucleoside , chemistry , oral administration , human immunodeficiency virus (hiv) , nucleoside analogue , virology , stereochemistry , biochemistry , medicine
Two new phosphonate 3TC prodrugs were synthesized and studied in MT‐4 cells as inhibitors of HIV replication. Their pharmacokinetic parameters were evaluated following intragastric administration in rabbits and oral administration in dogs. Both compounds were much less toxic than parent 3TC in cell cultures and could generate the active nucleoside in laboratory animals.