Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase.
N-3-Benzyloxycarbonylmethyl- and N-3-carboxymethyl-TBDMS-substituted nucleosides were synthesized and evaluated for activity against HIV replication. It was found that the N-3-carboxymethyl-TBDMS-substituted nucleosides were specific inhibitors of HIV-1 replication. They should be considered as members of a novel and original class of NNRTIs.
Chamorro
C
C
Instituto de Química Médica (C.S.I.C.), Juan de la Cierva 3, 28006-Madrid, Spain.
Lobatón
E
E
Bonache
M C
MC
De Clercq
E
E
Balzarini
J
J
Velázquez
S
S
San-Félix
A
A
Camarasa
M J
MJ
D004353:Drug Evaluation, Preclinical; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D015497:HIV-1 / Q000187:drug effects; D015498:HIV-2 / Q000187:drug effects; D006801:Humans; D009705:Nucleosides / Q000737:chemistry* / Q000494:pharmacology*; D017646:Organosilicon Compounds / Q000737:chemistry; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000821:virology
D009705:Nucleosides; D017646:Organosilicon Compounds; D018894:Reverse Transcriptase Inhibitors; C404749:tert-butyldimethylsilyl chloride; D054303:HIV Reverse Transcriptase