Department of Applied Chemistry, College of Science, China Agricultural University, Beijing, People's Republic of China.
Bioorg Med Chem Lett. 2011 Dec 1;21(23):7193-6. doi: 10.1016/j.bmcl.2011.09.068. Epub 2011 Sep 22.
Assuming that the water solubility of our previous hydrazone derivatives would improve after modification with sugars while keeping or modulating their notable biological activities, we designed and synthesized some glycosyl hydrazine and hydrazone derivatives. Bioassay results indicated that the antitumor activity of our previously prepared hydrazones reduced or disappeared after modification with sugars. On the contrary, some glycosyl derivatives displayed much better antifungal activity against selected fungi. Obviously, a small sugar can change the biological activity of hydrazones significantly.
假设我们之前的腙衍生物经过糖基化修饰后，其水溶性会提高，同时保持或调节其显著的生物活性，我们设计并合成了一些糖基肼和腙衍生物。生物测定结果表明，我们之前制备的腙经过糖基化修饰后，其抗肿瘤活性降低或消失。相反，一些糖基衍生物对选定的真菌显示出更好的抗真菌活性。显然，一个小糖基可以显著改变腙的生物活性。
