摘要：A series of 2-alkylthio-1-_4-(1-benzyl-2-ethyl-4-nitro-1H- -imidazol-5-yl)-piperazin-1-ylethanones (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 analogue 22 were synthesized from 4-nitro-5-piperazinyl imidazole derivative 1,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.Compound 2 showed inhibition of HIV-1 (EC50 0.45 mg mL–1) and HIV-2 (0.50 mg mL–1),while 9 showed inhibition of HIV-1 (EC50 2.48 mg mL–1,SI = 4).
