期刊
CHEMICAL & PHARMACEUTICAL BULLETIN
卷 56, 期 5, 页码 720-722出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.56.720
关键词
N-arylindole; anti-human immunodeficiency virus type 1; integrase inhibitor; synthesis
Eight simple N-arylindoles were designed, synthesized and evaluated as human immunodeficiency virus (HIV)-1 integrase inhibitors in vitro for the first time. Among these compounds, 3b, 3e and 3g demonstrated significant anti-HIV-1 integrase activity. Especially 3b showed the highest anti-HIV-1 integrase activity with EC50 value of 7.88 mu g/ml and TI value of 24.61. Meantime, some structure-activity relationships were also observed and will provide a new lead for design and discovery of more potent N-arylindoles as HIV-1 integrase inhibitors.
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