Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships |
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| Authors: | 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 |
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| Institution: | Neurogen Corporation, 35Northeast Industrial Road, Branford, CT 06405, USA. hzhao@nrgn.com |
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| Abstract: | 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. |
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