期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 44, 期 5, 页码 2190-2201出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2008.10.032
关键词
Acylthiocarbamates; HIV-1; Non-nucleoside reverse transcriptase inhibitors; Parallel synthesis
资金
- MURST (Cofinanziamento Nazionale)
- Fondazione Banca Carige
The structure-activity relationships (SARs) of acylthiocarbamates (ATCs), a new class of non-nucleoside HIV-1 reverse transcriptase inhibitors, have been expanded. Sixty-six new analogues were prepared by parallel solution-phase synthesis. In general. the potency of new ATCs was better than that of the first series and O-[2-phthalimidoethyl] 4-chlorophenyl(3-nitrobenzoyl) thiocarbamate turned out to be the most potent ATC so far synthesized (EC50 = 1.5 nM). Several ATCs were active at micromolar concentrations against HIV-1 strains carrying the RT Y181C mutation and one of them was also moderately active against the K103R variant. Docking simulations were carried out to rationalize the most relevant SARs. (C) 2008 Elsevier Masson SAS. All rights reserved.
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