Piperine amide analogs are synthesized by replacement of the piperidine moiety with different types of cyclic amines, including adamantyl and monoterpene‐derived fragments. The compounds are screened for activity against Mycobacterium tuberculosis H37Rv. The most potent compounds are the 1‐adamantyl and the monoterpene‐derived hybrids, which combine nanomolar antimycobacterial activity with low cytotoxicity against human cells. The presence of quaternary carbon atom as main structural requirement for anti‐TB activity is pointed out by a QSAR study. The most promising compound is the (+)‐isopinocampheylamine‐derived amide which is characterized with selectivity index of 1387.8.

中文翻译：

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具有抗分枝杆菌活性的合成胡椒碱酰胺类似物

胡椒碱酰胺类似物是通过用不同类型的环胺（包括金刚烷基和单萜衍生的片段）取代哌啶部分而合成的。筛选化合物对结核分枝杆菌H37Rv的活性。最有效的化合物是1-金刚烷基和单萜衍生的杂种，它们结合了纳摩尔的抗分枝杆菌活性和对人细胞的低细胞毒性。QSAR研究指出，存在季碳原子是抗结核活性的主要结构要求。最有前途的化合物是（+）-异opincampheylamine衍生的酰胺，其选择性指数为1387.8。