Nitroimidazoies, Part 4: Synthesis and anti-HIV activity of new 5-alkylsulfanyl and 5-(4 '-arylsulfonyl)piperazinyl-4-nitroimidazole derivatives

作者：Al Soud Yaseen A; Al Masoudi Najim A^*; De Clereq Erik; Paneccoque Christoph

来源：Heteroatom Chemistry, 2007, 18(4): 333-340.

DOI：10.1002/hc.20301

The development of new HIV nonnucleoside reverse transcriptase inhibitors (NNRTIs) offers the possibility of generating structures of increased potency. On this basis, a series of 5-alkylsulfanyl and 5-(4'-arylsulfonyl)piperazine derivatives of 1-phenyl-2-alkyl-4-nitroimidazoles 5-21 was synthesized with the aim to develop new NNRTIs. The new synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. Compounds 9 and 13, with an alkyl-sulfanyl group at C-5 of the 4-nitroimidazole backbone, showed inhibition of HIV-1 with EC50 4.04 mu g/mL and 2.37 mu g/mL, and therapeutic indexes (SI) of 17 and 13, respectively.

• 出版日期2007
• 单位河北医科大学