蛋白酪氨酸磷酸酶1B抑制剂的合成：模型验证与对接研究。
Synthesis of protein tyrosine phosphatase 1B inhibitors: model validation and docking studies.
作者信息
Saxena Anil K, Pandey Gyanendra, Gupta Swati, Singh Amar Bahadur, Srivastava Arvind K
机构信息
Central Drug Research Institute, Medicinal and Process Chemistry, Chattar Manzil Palace, Mahatma Gandhi Marg, Lucknow, Uttar Pradesh, India.
出版信息
Bioorg Med Chem Lett. 2009 Apr 15;19(8):2320-3. doi: 10.1016/j.bmcl.2009.02.058. Epub 2009 Feb 21.
The designed and synthesized 2-(4-methoxyphenyl) ethyl] acetamide derivatives (3a, 3b and 3c) were evaluated for their PTP1B inhibitory activity where they showed IC(50) values 69 microM, 87 microM and 71 microM, respectively. These results correlated well with the docking studies and in vivo screening of the compounds for their antidiabetic activity in SLM and STZ models.
对设计并合成的2-(4-甲氧基苯基)乙酰胺衍生物(3a、3b和3c)进行了蛋白酪氨酸磷酸酶1B(PTP1B)抑制活性评估，结果显示它们的半数抑制浓度(IC50)值分别为69微摩尔、87微摩尔和71微摩尔。这些结果与对接研究以及在链脲佐菌素(SLM)和链脲佐菌素(STZ)模型中对这些化合物抗糖尿病活性的体内筛选结果高度相关。
Zotero 插件