185525-88-6Relevant articles and documents
Synthesis and biological activities of spiroheterocyclic growth hormone secretagogues
Chen, Meng-Hsin,Pollard, Patrick P.,Patchett, Arthur A.,Cheng, Kang,Liente, Wei,Chan, Wanda W.-S.,Butler, Bridget,Jacks, Thomas M.,Smith, Roy G.
, p. 1261 - 1266 (2007/10/03)
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.
Peptidomimetic growth hormone secretagogues: Synthesis and biological activities of analogs varied at the indole nucleus of the prototypical spiropiperidine L-162,752
Nargund, Ravi P.,Chen, Meng-Hsin,Johnston, David B. R.,Barakat, Khaled J.,Tata, James R.,Cheng, Kang,Jacks, Thomas M.,Chan, Wanda W. -S,Wei, Liente,Butler, Bridget R.,Hickey, Gerard J.,Smith, Roy G.,Patchett, Arthur A.
, p. 1731 - 1736 (2007/10/03)
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 β-alanine amino side-chains led to a considerable loss of activity in the D-homophenylalanine and O-benzyl-D-serine series.