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用噁二唑硫酮杂环作为培氟沙星(1)的C3羧基电子等排体,得中间体C3噁二唑硫酮4(5),再将其与仲胺或取代苯胺及甲醛通过氨甲基化反应形成系列氟喹诺酮C3噁二唑硫酮曼尼希碱(6a～6j)目标化合物。用元素分析、1H NMR和MS测试技术确证了目标化合物的组成和结构。采用MTT法评价了目标化合物对体外培养人肝癌Hep-3B细胞生长的抑制活性。结果表明,10种目标化合物活性均显著高于对照化合物1的活性,并且脂肪胺曼尼希碱的活性高于芳香胺曼尼希碱的活性。
The oxadiazolethione 4 (5) was synthesized using the oxadiazolethione heterocycle as the C3 carboxylisostere of pefloxacin (1), which was then passed to the secondary or substituted aniline and formaldehyde Aminomethylation formed a series of fluoroquinolones C3 oxadiazole thione Mannich base (6a ~ 6j) target compounds. The composition and structure of the target compound were confirmed by elemental analysis, 1H NMR and MS test techniques. The inhibitory activity of the target compound on the growth of Hep-3B cells cultured in vitro was evaluated by MTT assay. The results showed that the activities of 10 target compounds were significantly higher than that of the control compound 1, and the activity of the amidoamine lipase was higher than that of the Mannich base of the aromatic amine.