Aaptamine derivatives with antifungal and anti-HIV-1 activities from the South China Sea sponge Aaptos aaptos.

作者: Hao-Bing Yu , Fan Yang , Fan Sun , Jing Li , Wei-Hua Jiao

DOI: 10.3390/MD12126003

关键词: South chinaAaptos aaptosBiologyMic valuesLactamSpongeAnti hiv 1AntifungalStereochemistryMoiety

摘要: Five new alkaloids of aaptamine family, compounds (1-5) and three known derivatives (6-8), have been isolated from the South China Sea sponge Aaptos aaptos. The structures all were unambiguously elucidated by spectroscopic analyses, as well comparison with literature data. Compounds 1-2 are characterized triazapyrene lactam skeleton, whereas 4-5 share an imidazole-fused moiety. These evaluated in antifungal anti-HIV-1 assays. 3, 7, 8 showed activity against six fungi, MIC values range 4 to 64 μg/mL. 7-8 exhibited activity, inhibitory rates 88.0% 72.3%, respectively, at a concentration 10 μM.

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