Synthesis and biological activities of spiroheterocyclic growth hormone secretagogues

被引:33
作者
Chen, MH [1 ]
Pollard, PP
Patchett, AA
机构
[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
[2] Merck Res Labs, Dept Biochem & Physiol, Rahway, NJ 07065 USA
关键词
D O I
10.1016/S0960-894X(99)00183-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and biological activities of a series of spiroheterocyclic growth hormone secretagogues are reported. Modification of the spiroindane part-structure of the prototypal secretagogue L-162,752 revealed that the spiroindane could be replaced with spirobenzodihydrothiophen derivatives to enhance not only in vitro potency but also oral activity. In this study non-aromatic D-2-amino-4-cyclohexylbutanoic analogs (8a-8d) were also identified to be active secretagogues, (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1261 / 1266
页数:6
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