<abstract xml:lang="en" xmlns="http://www.w3.org/1999/xhtml">A series of 2-alkylthio-1-[4-(1-benzyl-2-ethyl-4-nitro-1<italic>H</italic>-
-imidazol-5-yl)-piperazin-1-y]lethanones (<bold>3-9</bold>) and alkyl-
[4-(1-benzyl-2-ethyl-4-nitro-1<italic>H</italic>-imidazol-5-yl)-piperazin-
-1-yl)ketones (<bold>11-20</bold>) as well as the indole analogue <bold>22</bold>
were synthesized from 4-nitro-5-piperazinyl imidazole
derivative <bold>1</bold>, 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 <bold>2</bold> showed inhibition of
HIV-1 (EC50 0.45 mg mL-1) and HIV-2 (0.50 mg mL-1),
while <bold>9</bold> showed inhibition of HIV-1 (EC50 2.48 mg mL-1,
SI = 4).</abstract>

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).

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

Department of Chemistry College of Science, University of Al al-Bayt Al-Mafraq, Jordan

Fachbereich Chemie, Universität Konstanz, Postfach 5560, D-78457 Konstanz Germany

College of Science Department of Chemistry, University of Sulaimany, Iraq

Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium

Acta Pharmaceutica

A series of 2-alkylthio-1-[4-(1-benzyl-2-ethyl-4-nitro-1H-
-imidazol-5-yl)-piperazin-1-y]lethanones (3-9) and...

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

Publié en ligne: 28 déc. 2007

Pages: 379 - 393

DOI: https://doi.org/10.2478/v10007-007-0031-7

Mots clés
anti-HIV djelovanje, 4-nitroimidazoli, NNRTIs, piperazin

This content is open access.

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

Publié en ligne: 28 déc. 2007

Pages: 379 - 393

DOI: https://doi.org/10.2478/v10007-007-0031-7

Mots clésanti-HIV djelovanje, 4-nitroimidazoli, NNRTIs, piperazin

This content is open access.

Mots clés
anti-HIV djelovanje, 4-nitroimidazoli, NNRTIs, piperazin