Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase

C Chamorro; E Lobatón; M C Bonache; E De Clercq; J Balzarini; S Velázquez; A San-Félix; M J Camarasa

doi:10.1016/s0960-894x(01)00635-7

Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase

Bioorg Med Chem Lett. 2001 Dec 3;11(23):3085-8. doi: 10.1016/s0960-894x(01)00635-7.

Authors

C Chamorro¹, E Lobatón, M C Bonache, E De Clercq, J Balzarini, S Velázquez, A San-Félix, M J Camarasa

Affiliation

¹ Instituto de Química Médica (C.S.I.C.), Juan de la Cierva 3, 28006-Madrid, Spain.

PMID: 11714616
DOI: 10.1016/s0960-894x(01)00635-7

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Drug Evaluation, Preclinical
HIV Reverse Transcriptase / antagonists & inhibitors*
HIV-1 / drug effects
HIV-2 / drug effects
Humans
Nucleosides / chemistry*
Nucleosides / pharmacology*
Organosilicon Compounds / chemistry
Reverse Transcriptase Inhibitors / chemistry*
Reverse Transcriptase Inhibitors / pharmacology*
Structure-Activity Relationship
Tumor Cells, Cultured / virology

Substances

Nucleosides
Organosilicon Compounds
Reverse Transcriptase Inhibitors
tert-butyldimethylsilyl chloride
HIV Reverse Transcriptase