Synthesis and SAR of substituted tetrahydrocarbazole derivatives as new NPY-1 antagonists

被引:38
作者
Di Fabio, R [1 ]
Giovannini, R [1 ]
Bertani, B [1 ]
Borriello, M [1 ]
Bozzoli, A [1 ]
Donati, D [1 ]
Falchi, A [1 ]
Ghirlanda, D [1 ]
Leslie, CP [1 ]
Pecunioso, A [1 ]
Rumboldt, G [1 ]
Spada, S [1 ]
机构
[1] GlaxoSmithKline Inc, Med Res Ctr, I-37135 Verona, Italy
关键词
NPY-1; antagonists; GPCR;
D O I
10.1016/j.bmcl.2005.11.104
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The SAR of a new series of tetrahydrocarbazole derivatives is described: the appropriate decoration of this template led to the identification of a new class of NPY-1 antagonists showing good in vitro potency and a promising in vivo pharmacokinetic profile in rat. (C) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1749 / 1752
页数:4
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