In this study, we present the discovery and pharmacological characterization of a new series of 6-piperazinyl-7-azaindoles. These compounds demonstrate potent antagonism and selectivity against the 5-HT₆ receptor. Our research primarily focuses on optimizing the lead structure and investigating the structure–activity relationship (SAR) of these compounds. Our main objective is to improve their activity and selectivity against off-target receptors.

Overall, our findings contribute to the advancement of novel compounds targeting the 5-HT₆ receptor. Compound 29 exhibits significant promise in terms of pharmacological, physicochemical, and ADME (Absorption, Distribution, Metabolism, and Excretion) properties. Consequently, it merits thorough exploration as a potential drug candidate due to its favorable activity profile and successful outcomes in a range of in vivo experiments.

在这项研究中，我们介绍了一系列新的 6-哌嗪基-7-氮杂吲哚的发现和药理学表征。这些化合物表现出对 5-HT ₆受体的有效拮抗作用和选择性。我们的研究主要集中于优化先导结构并研究这些化合物的构效关系（SAR）。我们的主要目标是提高它们对脱靶受体的活性和选择性。

总的来说，我们的研究结果有助于开发针对 5-HT ₆受体的新型化合物。化合物29在药理学、理化和 ADME（吸收、分布、代谢和排泄）特性方面表现出巨大的前景。因此，由于其良好的活性特征和一系列体内实验的成功结果，它值得作为潜在的候选药物进行彻底的探索。