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

VernacularTitle: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
Author: Dong LIU ¹ ; Ting-ting GUO ¹ ; Wei-ping WANG ¹ ; Xiao-liang WANG ¹ ; Bai-ling XU ¹
Author Information

1. Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Publication Type:ORIGINAL ARTICLES
Keywords: Kv2.1 inhibitor; 2,3-dihydro-1H-pyrrolo[3,2-c]quinoline; 2,3,5,9b-tetrahydro-1H-pyrrolo[3,2-c] quinoline
From: Acta Pharmaceutica Sinica 2016;51(5):762-
CountryChina
Language:Chinese
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 IC₅₀ values of 10.2 and 9.0 μmol·L^-1, respectively.