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

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.

Citation

He Zhao, Andrew Thurkauf, Xiaoshu He, Kevin Hodgetts, Xiaoyan Zhang, Stanislaw Rachwal, Renata X Kover, Alan Hutchison, John Peterson, Andrzej Kieltyka, Robbin Brodbeck, Renee Primus, Jan W F Wasley. Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships. Bioorganic & medicinal chemistry letters. 2002 Nov 4;12(21):3105-9

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PMID: 12372512

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