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[2,3-二氢-1H-吡咯并[3,2-c]喹啉及2,3,5,9b-四氢-1H-吡咯并[3,2-c]喹啉衍生物:合成及其对Kv2.1的抑制活性]

[2,3-Dihydro-1H-pyrrolo[3,2-c]quinoline and 2,3,5,9b-tetrahydro-1H-pyrrolo[3,2-c]-quinoline derivatives:synthesis and their inhibitory activity against Kv2.1].

作者信息

Liu Dong, Guo Ting-ting, Wang Wei-ping, Wang Xiao-liang, Xu Bai-ling

出版信息

Yao Xue Xue Bao. 2016 May;51(5):762-9.

Abstract

Fourteen new compounds with 2,3-dihydro-1H-pyrrolo[3,2-c]-quinoline or 2,3,5,9b-tetrahydro-1H-pyrrolo[3,2-c]quinoline scaffold were designed and synthesized, and their inhibitory activities against Kv2.1 were evaluated. As a result,2,3-dihydro-1H-pyrrolo[3,2-c]quinoline derivatives 3a and 5a were identified as potent inhibitors of Kv2.1 with IC(50) values of 10.2 and 9.0 μmol·L(-1), respectively.

摘要

设计并合成了14种具有2,3-二氢-1H-吡咯并[3,2-c]喹啉或2,3,5,9b-四氢-1H-吡咯并[3,2-c]喹啉骨架的新化合物,并评估了它们对Kv2.1的抑制活性。结果,2,3-二氢-1H-吡咯并[3,2-c]喹啉衍生物3a和5a被鉴定为Kv2.1的有效抑制剂,IC(50)值分别为10.2和9.0 μmol·L(-1)。

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