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…

Index: Bioorganic and Medicinal Chemistry Letters, , vol. 12, # 21 p. 3105 - 3109

Full Text: HTML

Citation Number: 19

Abstract

... Bioorganic & Medicinal Chemistry Letters. ... Screening of a chemical library uncovered 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2,3-dihydro-indol-1-yl)-ethanone 1 showing high affinity binding for D 4 (1.6 nM), relatively modest binding for D 2 (690 nM) and significant affinity for ...

Related Articles:

Synthesis, biological evaluation and SAR studies of benzimidazole derivatives as H 1-antihistamine agents

[Wang, Xiao Jian; Xi, Mei Yang; Fu, Ji Hua; Zhang, Fu Rong; Cheng, Gui Fang; Yin, Da Li; You, Qi Dong Chinese Chemical Letters, 2012 , vol. 23, # 6 p. 707 - 710]

Asymmetric hydrogenation of 3-alkylidene-2-piperidones using Noyori's catalyst. Effect of N-substituents on the enantioselectivity

[Chung, John Y. L.; Zhao, Dalian; Hughes, David L.; McNamara, James M.; Grabowski, Edward J. J.; Reider, Paul J. Tetrahedron Letters, 1995 , vol. 36, # 41 p. 7379 - 7382]

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

[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]

Non-peptide fibrinogen receptor antagonists. 2. Optimization of a tyrosine template as a mimic for Arg-Gly-Asp

[Journal of Medicinal Chemistry, , vol. 37, # 16 p. 2537 - 2551]

Non-peptide fibrinogen receptor antagonists. 2. Optimization of a tyrosine template as a mimic for Arg-Gly-Asp

[Journal of Medicinal Chemistry, , vol. 37, # 16 p. 2537 - 2551]

More Articles...