Metal-assisted synthesis of unsymmetrical magnolol and honokiol analogs and their biological assessment as GABAA receptor ligands by Biotage Initiator耐士科技

2015/02/09   下载量： 4 次

方案摘要

方案下载
应用领域 制药/生物制药
检测样本 化药新药研发
检测项目 其他>方法开发
参考标准 GB/T 8****

We present the synthesis of new derivatives of natural products magnolol (1) and honokiol (2) and their evaluation as allosteric ligands for modulation of GABAA receptor activity. New derivatives were prepared via metal assisted cross-coupling reactions in two consecutive steps. Compounds were tested by means of two-electrode voltage clamp electrophysiology at the a1b2c2 receptor subtype at low GABA concentrations.We have identified several compounds enhancing GABA induced current (IGABA) in the range similar or even higher than the lead structures. At 3 lM, compound 8g enhanced IGABA by factor of 443, compared to 162 and 338 of honokiol and magnolol, respectively. Furthermore, 8g at EC10–20 features a much bigger window of separation between the a1b2c2 and the a1b1c2 subtypes compared to honokiol, and thus improved subtype selectivity.

方案下载
上一篇 耐士科技：使用Biotage Isolera快速纯化液相制备色谱从库拉索芦荟叶皮提取天然的磷酸二酯酶抑制剂by耐士科技
下一篇 Microwave assisted synthesis and characterization of end functionalized poly(propylene oxide) as model compounds by Biotage Initiator耐士科技

文献贡献者

上海鑫欣生物科技有限公司
银牌会员 丨 第14年
查看全部资料
相关仪器 更多
相关方案
更多

相关产品

当前位置： 上海鑫欣生物 方案 Metal-assisted synthesis of unsymmetrical magnolol and honokiol analogs and their biological assessment as GABAA receptor ligands by Biotage Initiator耐士科技

关注

拨打电话

留言咨询