摘要
目的:合成两个新的化合物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[3,3,3,01,5]十一碳烷3a和3b,并对其抗炎活性进行研究。方法:先合成γ-氨丙基杂氮硅三环,对其氨丙基上氨基进行异氰酸酯化得到。通过环氧化酶(COX)抑制剂体外试剂盒,设40、80、160μg/mL三个浓度对化合物进行抗炎实验。结果:合成的目标物结构经IR、MS、1H-NMR及元素分析验证确认;对COX-1抑制活性最高的是化合物3a在160μg/mL时,抑制率为33.34%;抑制活性最低的是3b在40μg/mL时,抑制率为1.67%;对COX-2抑制活性最高的是化合物3a在160μg/mL时,抑制率为20.22%,抑制活性最低的是3b在40μg/mL时,抑制率为1.78%。结论:化合物3a具有一定的COX抑制活性,在三个浓度条件下,随浓度的升高而活性增强。
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 theγ-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,MS1,H-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 40μg/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 40μg/mL.Conclusion：Compound 3a has some degree COX inhibition,and with the rise of the concentration,the activity is increased.
出处
《温州医学院学报》
CAS
2010年第4期330-332,共3页
Journal of Wenzhou Medical College
基金
浙江省自然科学基金资助项目(Y204087)
