A specific and direct comparison of the trifluoromethyl and pentafluoro sulfanyl groups on the selective dopamine D3 antagonist 3-(3-{[4-methyl-5-(4-methyl-1,3-oxazol-5-yl)-4H-1,2,4-triazol-3-yl]thio}propyl)-1-phenyl-3-azabicyclo[3.1.0] hexane template

被引:18
作者
Micheli, Fabrizio [1 ]
Andreotti, Daniele [1 ]
Braggio, Simone [1 ]
Checchia, Anna [1 ]
机构
[1] GlaxoSmithKline Med Res Ctr, Neurosci Ctr Excellence, I-37135 Verona, Italy
关键词
Dopamine D3; Antagonist; DMPK; Pentafluorosulfanyl; Trifluoromethyl; RECEPTOR ANTAGONISTS; POTENT; SERIES; D3;
D O I
10.1016/j.bmcl.2010.06.018
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A direct and specific comparison of a trifluoromethyl group with the corresponding pentafluorosulfanyl group is made in terms of primary affinity and pharmacokinetic properties. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4566 / 4568
页数:3
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