Design, synthesis, and structure-activity relationships of indole-3-carboxamides as novel water soluble cannabinoid CB1 receptor agonists
Design, synthesis, and structure-activity relationships of indole-3-carboxamides as novel water soluble cannabinoid CB1 receptor agonists
复制标题
DOI：
10.1039/c0md00022a
复制
发表时间：
2010-07-01
期刊：
影响因子：
--
通讯作者：
Walker, Glenn
中科院分区：
文献类型：
--
作者：
Adam, Julia M.;Cairns, Jim;Walker, Glenn
使用高通量筛选方法鉴定了一种新型CBI受体激动剂先导系列。初始筛选提供了单一确认的命中，具有差的水溶性。探索了结构变化，目的是引入水溶性和提高效力。这导致了一种有效的水溶性CBI受体激动剂--CBI 28611的发现，其被选择作为潜在的静脉内镇痛剂用于临床评价。
A novel CBI receptor agonist lead series was identified using a high-throughput screening approach. The initial screen afforded a single confirmed hit with poor water solubility. Structural variations were explored with the aim of introducing water solubility and improving potency. This led to the discovery of Org 28611, a potent, water soluble CBI receptor agonist, which was selected for clinical evaluation as a potential intravenous analgesic agent.