γ-（甲基取代苯氨基甲酰胺基）－丙基－2,8,9-三氧杂－5-氮杂－1-硅杂三环[3,3,3,0(上标 1, 5)]十一碳烷的合成及其活性研究

Objective: To synthesize two novel silatrane compounds (3a and 3b) and study their COX inhibition. Method: The compounds (3a and 3b) were synthesized by the isocyanation of γ-aminopropyl silatrane. The anti-inflammatory activity was at first evaluated in vitro with three different concentrations (408, 0, 160 μg/mL). The arnido on the the γ-amino-propyl silatranes was obtained through isocyanate. Via COX enzyme inhibitor in vitro kit, three concentrations were set to carry out experiment. Results: The product was identified by IR, MS, 1H-NMR and elemental analysis: Compound 3a showed the highest inhibitory activity of COX-1 in 160 μg/mL with the inhibition rate of 33.34%, while 3b displayed the lowest activity in 40 μg/mL with the inhibition rate of 1.67%. As to the inhibitory activity of COX-2, 3a had a inhibition rate of 20.22% in 160 μg/mL, and 3b was 1.78% in 40 μg/mL. Conclusion: Compound 3a has some degree COX inhibition, and with the rise of the concentration, the activity is increased.