Peptidomimetic Growth Hormone Secretagogues: Synthesis And Biological Activities Of Analogs Varied At The Indole Nucleus Of The Prototypical Spiropiperidine L-162,752

SAR studies around the indole nucleus of the prototypical peptidomimetic L-162,752 revealed that the D-Trp could be replaced with 3-phenylpropyl-D-glycine and O-benzyl-D-serine to provide secretagogues with comparable intrinsic activity but with significantly better oral activity in dogs. Use of dimethyl beta-alanine amino side-chains led to a considerable loss of activity in the D-homophenylalanine and O-benzyl-D-serine series. Copyright (C) 1996 Elsevier Science Ltd