A.E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences, 1 Favorsky Street, 664033 Irkutsk, Russia.
Irkutsk Antiplague Research Institute of Siberia and Far East, 78 Trilisser Street, 664047 Irkutsk, Russia.
Int J Mol Sci. 2023 Jun 9;24(12):9965. doi: 10.3390/ijms24129965.
The biologically active compound 3-aminopropylsilatrane (a compound with a pentacoordinated silicon atom) underwent an aza-Michael reaction with various acrylates and other Michael acceptors. Depending on the molar ratio, the reaction yielded Michael mono- or diadducts (11 examples) containing functional groups (silatranyl, carbonyl, nitrile, amino, etc.). These compounds were characterized via IR and NMR spectroscopy, mass spectrometry, X-ray diffraction, and elemental analysis. Calculations (using in silico, PASS, and SwissADMET online software) revealed that the functionalized (hybrid) silatranes were bioavailable, druglike compounds that exhibited pronounced antineoplastic and macrophage-colony-stimulating activity. The in vitro effect of silatranes on the growth of pathogenic bacteria (, , and ) was studied. It was found that the synthesized compounds exerted inhibitory and stimulating effects in high and low concentrations, respectively.
生物活性化合物 3-氨丙基硅烷（一种具有五配位硅原子的化合物）与各种丙烯酸酯和其他迈克尔受体发生了氮杂迈克尔加成反应。根据摩尔比，反应生成了含有功能基团（硅烷醇基、羰基、腈基、氨基等）的迈克尔单加或双加产物（11 个实例）。这些化合物通过红外和核磁共振波谱、质谱、X 射线衍射和元素分析进行了表征。计算（使用计算机辅助软件、PASS 和 SwissADMET 在线软件）表明，功能化（杂化）硅烷醇是可生物利用的、类药性化合物，具有明显的抗肿瘤和巨噬细胞集落刺激活性。研究了硅烷醇对致病菌（、和）生长的体外影响。结果发现，合成的化合物在高浓度和低浓度下分别表现出抑制和刺激作用。
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