616882-05-4Relevant academic research and scientific papers
3-SPIROCYCLIC PIPERIDINE DERIVATIVES AS GHRELIN RECEPTOR AGONISTS
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Page/Page column 78, (2012/12/13)
The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicam
Structure activity studies of the serine-AIB dipeptide domain in 2,3-dihydroisothiazole based growth hormone secretagogues
Evers, Britta,Ruehter, Gerd,Berg, Martina,Dodge, Jeffrey A.,Hankotius, Dirk,Hary, Ulrike,Jungheim, Louis N.,Mest, Hans-Juergen,De La Nava, Eva-Maria Martin,Mohr, Michael,Muehl, Brian S.,Petersen, Soenke,Sommer, Birgit,Riedel-Herold, Grit,Tebbe, Mark J.,Thrasher, Kenneth J.,Voelkers, Silke
, p. 6748 - 6762 (2007/10/03)
A series of growth hormone secretagogues (GHSs) based on 2,3-dihydroisothiazole has been synthesized in the search for a potential treatment of growth hormone deficiency or frailty in the elderly. This paper describes the evaluation of the SAR of the benzyl-d-Ser-aminoisobutyric acid dipeptide fragment. Introduction of substituents in the peptide backbone and in the phenyl ring has been investigated, as well as replacements for the benzyl group and for the AIB residue. A number of modifications resulted in enhanced potency over the parent benzyl-d-Ser-AIB derivative.
