Author:
Al-Soud Yaseen,Al-Masoudi Najim,Hassan Hamed,De Clercq Erik,Pannecouque Christophe
Abstract
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).
Subject
Pharmaceutical Science,Pharmacology,General Medicine
Reference28 articles.
1. Pharmacologic studies of the anti-tumor agent 5-(dimethyltriazeno)imidazole-4-carboxamide;T. Loo;Cancer Res.,1968
2. Synthesis of an (iodovinyl) misonidazole derivative for hypoxia imaging;J. Biskupiak;J. Med. Chem.,1991
3. Synthesis and antifungal activity of a series of difluorotritylimidazoles;J. Bartroli;Arzneim.-Forsch.,1992
4. A novel thermal rearrangement of 1-tritylimidazoles;I. Saji;Heterocycles,1981
5. Antiparasitic nitroimidazoles. 3. Synthesis of 2-(4-carboxystyryl)-5-nitro-1-vinylimidazole and related compounds;W. Ross;J. Med. Chem.,1973
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