Indoline and piperazine containing derivatives as a novel class of mixed D 2/D 4 receptor antagonists. Part 1: identification and structure–activity relationships

H Zhao, A Thurkauf, X He, K Hodgetts, X Zhang…

文献索引：Zhao, He; Thurkauf, Andrew; He, Xiaoshu; Hodgetts, Kevin; Zhang, Xiaoyan; Rachwal, Stanislaw; Kover, Renata X.; Hutchison, Alan; Peterson, John; Kieltyka, Andrzej; Brodbeck, Robbin; Primus, Renee; Wasley, Jan W.F. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 21 p. 3105 - 3109

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被引用次数: 19

摘要

Optimization of the lead compound 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2, 3-dihydro- indol-1-yl)-ethanone 1 by systematic structure–activity relation (SAR) studies lead to two potent compounds 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2-methy-2, 3-dihydro-indol-1-yl)- ethanone 2n and 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2-methy-2, 3-dihydro-indol-1-yl)- ethanone 7b. Their related synthesis was also reported.