Résumé
The bis(
S-acetyl-2-thioethyl) phosphotriester derivative of 2′,3′-didehydro-2′,3′-dideoxythymidine has been synthesized and evaluated for its inhibitory effects on the replication of HIV-1 in several cell culture systems. This pronucleotide showed potent anti-HIV activity and proved to be significantly superior to the parent nucleoside with regard to the antiviral efficiency.
The
in vitro antiviral efficiency of d4T can be enhanced by the use of the corresponding mononucleoside phosphotriester incorporating the esterase-labile transient phosphate-protecting group, namely,
S-acetyl-2-thioethyl (MeSATE).