Synthetic piperine amide analogs with antimycobacterial activity,Chemical Biology & Drug Design

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Synthetic piperine amide analogs with antimycobacterial activity
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2017-11-27 00:45:51 , DOI: 10.1111/cbdd.13140
Irena Philipova ₁ , Violeta Valcheva ₂ , Rositsa Mihaylova ₃ , Mina Mateeva ₃ , Irini Doytchinova ₃ , Georgi Stavrakov _{1,

3}

Affiliation

A series of Piperine amide analogues are synthesized by replacing piperidine moiety with different types of cyclic amines, including cyclohexyl, bicyclo[2.2.1]heptyl, adamantyl, and monoterpene-derived fragments. The hybrid analogues with 1-adamantyl and the monoterpene fragments displayed nanomolar antimycobacterial activity with low cytotoxicity against human cells. A QSAR study pointed out the presence of quaternary carbon atom as main structural requirement for the activity. The most promising compound is the (+)-isopinocampheylamine-derived amide, with selectivity index of 1387.8.

中文翻译：

具有抗分枝杆菌活性的合成胡椒碱酰胺类似物

通过用不同类型的环胺（包括环己基，双环[2.2.1]庚基，金刚烷基和单萜衍生的片段）取代哌啶部分，可以合成一系列哌啶酰胺类似物。具有1-金刚烷基和单萜片段的杂合类似物表现出纳摩尔抗分枝杆菌活性，对人细胞的细胞毒性低。一项QSAR研究指出，季碳原子的存在是该活性的主要结构要求。最有前途的化合物是（+）-异opincampcampylylamine衍生的酰胺，选择性指数为1387.8。

更新日期：2017-11-27

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