Synthesis and biological activities of spiroheterocyclic growth hormone secretagogues
作者:Meng-Hsin Chen、Patrick P. Pollard、Arthur A. Patchett、Kang Cheng、Liente Wei、Wanda W.-S. Chan、Bridget Butler、Thomas M. Jacks、Roy G. Smith
DOI:10.1016/s0960-894x(99)00183-3
日期:1999.5
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
报道了一系列螺杂环生长激素促分泌剂的合成和生物学活性。原型促分泌素L-162,752的螺茚满烷部分结构的修饰表明,可用螺苯并二氢噻吩衍生物代替螺茚满,不仅可以增强体外效力,而且还可以增强口服活性。在这项研究中,非芳香族D-2-氨基-4-环己基丁酸类似物(8a-8d)也被确定为活性促泌剂。