基于苯基哌嗪的肽模拟生长激素促分泌剂的合成及生物活性
Synthesis and biological activities of phenyl piperazine-based peptidomimetic growth hormone secretagogues.
作者信息
Barakat K J, Cheng K, Chan W W, Butler B S, Jacks T M, Schleim K D, Hora D F, Hickey G J, Smith R G, Patchett A A, Nargund R P
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 1998 Jun 2;8(11):1431-6. doi: 10.1016/s0960-894x(98)00238-8.
A new class of potent, orally active phenyl piperazine-based GH secretagogues have been discovered from attempts to mimic the arrangement of the phenyl substituent in the spiroindanyl piperidine and spiroindoline sulfonamide privileged structures of 4 and 1, respectively. The best of these compounds, 18 (EC50 = 2.8 nM) is nearly as potent as MK-0677 for releasing GH from rat pituitary cells.
通过尝试模拟分别具有4和1的螺茚满基哌啶及螺茚满啉磺酰胺优势结构中苯基取代基的排列方式，已发现一类新型强效、口服活性的基于苯基哌嗪的生长激素促分泌素。这些化合物中最优者，即化合物18（半数有效浓度EC50 = 2.8 nM），在促使大鼠垂体细胞释放生长激素方面，其效力几乎与MK - 0677相当。
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