Abstract
Synthesis, biological activities and decomposition kinetics of novel phosphotriester derivatives of 3'-azido-2',3'-dideoxythymidine (AZT) bearing a S-tButyl-2-thioethyl (tBuSATE) group and L-tyrosinyl residues are reported. All the derivatives appeared to be potent inhibitors of HIV-1 replication in various cell culture experiments. The proposed decomposition process of these mixed phosphotriesters may involve successively an esterase and then a phosphodiesterase activation.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Anti-HIV Agents / chemical synthesis*
-
Anti-HIV Agents / chemistry
-
Anti-HIV Agents / pharmacology*
-
Cells, Cultured
-
Drug Design
-
Drug Stability
-
Esters / chemical synthesis
-
Esters / chemistry
-
Esters / pharmacology
-
HIV-1 / drug effects
-
HIV-1 / physiology
-
Humans
-
Prodrugs / chemical synthesis*
-
Prodrugs / chemistry
-
Prodrugs / pharmacology*
-
Virus Replication / drug effects
-
Zidovudine / analogs & derivatives*
-
Zidovudine / chemical synthesis
-
Zidovudine / pharmacology
Substances
-
Anti-HIV Agents
-
Esters
-
Prodrugs
-
Zidovudine