Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, No. 325 Guohe Road, Shanghai 200433, China.
Bioorg Med Chem Lett. 2012 Sep 15;22(18):5849-52. doi: 10.1016/j.bmcl.2012.07.087. Epub 2012 Aug 1.
In order to search for drugs with excellent anti-inflammatory activities, a series of novel sinomenine derivatives were designed, synthesized, and evaluated for their inhibition activities against NF-κB activation induced by lipopolysaccharide (LPS). Compared with the natural parent sinomenine, compounds 2a-w showed higher activity, while compounds 1a-o showed similar activity against NF-κB. Moreover, a molecular model for the binding between compound 2v and the active site of p50 was provided on the basis of the computational docking results.
为了寻找具有优异抗炎活性的药物，设计、合成了一系列新型盐酸青藤碱衍生物，并评价了它们对脂多糖（LPS）诱导的 NF-κB 激活的抑制活性。与天然母体盐酸青藤碱相比，化合物 2a-w 表现出更高的活性，而化合物 1a-o 对 NF-κB 的活性相似。此外，根据计算对接结果，提供了化合物 2v 与 p50 活性位点结合的分子模型。
