喹啉并吡咯烷和二氢喹啉并吡咯烷衍生物的合成及Kv2.1抑制活性评价

2,3-Dihydro-1H-pyrrolo3,2-cquinoline and 2,3,5,9b-tetrahydro-1Hpyrrolo3,2-c-quinoline derivatives: synthesis and their inhibitory activity against Kv2.1

摘要: 本文合成了新结构的喹啉并吡咯烷和二氢喹啉并吡咯烷类化合物14 个, 评价了化合物对钾离子通道亚型Kv2.1 的抑制活性。发现二氢喹啉并吡咯烷类化合物3a 和5a 对Kv2.1 具有抑制活性, IC₅₀值分别为10.2 和9.0 μmol·L^-1。本文对构效关系进行了初步分析, 研究结果为进一步结构改造提供了启示。

Abstract: Fourteen new compounds with 2,3-dihydro-1H-pyrrolo3,2-c-quinoline or 2,3,5,9b-tetrahydro- 1H-pyrrolo3,2-cquinoline scaffold were designed and synthesized, and their inhibitory activities against Kv2.1 were evaluated. As a result, 2,3-dihydro-1H-pyrrolo3,2-cquinoline derivatives 3a and 5a were identified as potent inhibitors of Kv2.1 with IC₅₀ values of 10.2 and 9.0 μmol·L^-1, respectively.