Synthesis and biological activities of spiroheterocyclic growth hormone secretagogues.
作者信息
Chen M H, Pollard P P, Patchett A A, Cheng K, Wei L, Chan W W, Butler B, Jacks T M, Smith R G
机构信息
Medicinal Chemistry Department, Merck Research Laboratories, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 1999 May 3;9(9):1261-6. doi: 10.1016/s0960-894x(99)00183-3.
Abstract
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.
摘要
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