Synthesis and biological activities of camphor-based non-peptide growth hormone secretagogues

被引:20
|
作者
Nargund, RP [1 ]
Barakat, KH [1 ]
Cheng, K [1 ]
Chan, WWS [1 ]
Butler, BR [1 ]
Smith, RG [1 ]
Patchett, AA [1 ]
机构
[1] MERCK & CO INC,MERCK SHARP & DOHME RES LABS,DEPT PHYSIOL,RAHWAY,NJ 07065
关键词
D O I
10.1016/0960-894X(96)00213-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and growth hormone (GH) releasing activities of a novel series of camphor-based non-peptide GH secretagogues is presented. Use of the (R)-nipecotic acid amino side-chain and N-terminal derivatization of it with an (R)-(2-hydroxy)propyl group provided a potent secretagogue 18 (EC(50) = 90 nM). An o-tolyl piperazine was identified as a good replacement for the spiroindanyl piperidine. Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码:1265 / 1270
页数:6
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