scholarly journals Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents

2017 ◽  
Vol 60 (15) ◽  
pp. 6528-6547 ◽  
Author(s):  
Valeria Famiglini ◽  
Giuseppe La Regina ◽  
Antonio Coluccia ◽  
Domiziana Masci ◽  
Andrea Brancale ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Broad Spectrum ◽  
Reverse Transcriptase Inhibitors ◽  
Nucleoside Reverse Transcriptase Inhibitors ◽  
Anti Hiv ◽  
Hiv 1

scholarly journals Synthesis, Anti-HIV Activity, and Metabolic Stability of New Alkenyldiarylmethane HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors

2005 ◽  
Vol 48 (19) ◽  
pp. 6140-6155 ◽  
Author(s):  
Bo-Liang Deng ◽  
Tracy L. Hartman ◽  
Robert W. Buckheit, ◽  
Christophe Pannecouque ◽  
Erik De Clercq ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Metabolic Stability ◽  
Reverse Transcriptase Inhibitors ◽  
Nucleoside Reverse Transcriptase Inhibitors ◽  
Anti Hiv ◽  
Hiv 1

scholarly journals New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors

2014 ◽  
Vol 80 ◽  
pp. 101-111 ◽  
Author(s):  
Valeria Famiglini ◽  
Giuseppe La Regina ◽  
Antonio Coluccia ◽  
Sveva Pelliccia ◽  
Andrea Brancale ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Broad Spectrum ◽  
Reverse Transcriptase Inhibitors ◽  
Nucleoside Reverse Transcriptase Inhibitors ◽  
Hiv 1

scholarly journals Indolylarylsulfones Carrying a Heterocyclic Tail as Very Potent and Broad Spectrum HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors

2014 ◽  
Vol 57 (23) ◽  
pp. 9945-9957 ◽  
Author(s):  
Valeria Famiglini ◽  
Giuseppe La Regina ◽  
Antonio Coluccia ◽  
Sveva Pelliccia ◽  
Andrea Brancale ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Broad Spectrum ◽  
Reverse Transcriptase Inhibitors ◽  
Nucleoside Reverse Transcriptase Inhibitors ◽  
Hiv 1

scholarly journals Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivatives

2007 ◽  
Vol 57 (4) ◽  
pp. 379-393 ◽  
Author(s):  
Yaseen Al-Soud ◽  
Najim Al-Masoudi ◽  
Hamed Hassan ◽  
Erik De Clercq ◽  
Christophe Pannecouque
Keyword(s):  
Reverse Transcriptase ◽  
Imidazole Derivative ◽  
Reverse Transcriptase Inhibitors ◽  
Nucleoside Reverse Transcriptase Inhibitors ◽  
Anti Hiv ◽  
Hiv 1

Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivativesA series of 2-alkylthio-1-[4-(1-benzyl-2-ethyl-4-nitro-1H- -imidazol-5-yl)-piperazin-1-y]lethanones (3-9) and alkyl- [4-(1-benzyl-2-ethyl-4-nitro-1H-imidazol-5-yl)-piperazin- -1-yl)ketones (11-20) as well as the indole analogue22were synthesized from 4-nitro-5-piperazinyl imidazole derivative1, with the aim to develop newly non-nucleoside reverse transcriptase inhibitors (NNRTIs). The newly synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. Compound2showed inhibition of HIV-1 (EC50 0.45 mg mL-1) and HIV-2 (0.50 mg mL-1), while9showed inhibition of HIV-1 (EC502.48 mg mL-1, SI = 4).

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