A 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 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).