Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivatives
Keyword(s):
Anti Hiv
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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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