介绍了已测试其生物活性的海藻酸类似物的全面调查。具体来说,这篇综述(1)根据相对活动量表收集和比较了100多个海象科动物,(2)暴露了优化红藻氨酸受体亲和力所需的结构特征,和(3)提出了创建下一代KA类似物的设计规则。文献SAR数据进行了系统分析,并与最新的晶体学研究相结合。鉴于对神经活性分子的重新兴趣,这篇综述旨在帮助指导有机合成实验室的工作,以及通知新人KA/GluK研究。
A comprehensive survey of kainic acid analogs that have been tested for their biological activity is presented. Specifically, this review (1) gathers and compares over 100 kainoids according to a relative activity scale, (2) exposes structural features required to optimize affinity for kainate receptors, and (3) suggests design rules to create next-generation KA analogs. Literature SAR data are analyzed systematically and combined with the most recent crystallographic studies. In view of the renewed interest in neuroactive molecules, this review aims to help guide the efforts of organic synthesis laboratories, as well as to inform newcomers to KA/GluK research.