Author/Authors :
Britta Evers، نويسنده , , Gerd Ruehter، نويسنده , , Martina Berg، نويسنده , , Jeffrey A. Dodge، نويسنده , , Dirk Hankotius، نويسنده , , Ulrike Hary، نويسنده , , Louis N. Jungheim، نويسنده , , Hans-Juergen Mest، نويسنده , , Eva-Maria Martin de la Nava، نويسنده , , Michael Mohr، نويسنده , , Brian S. Muehl، نويسنده , , Soenke Petersen، نويسنده , , Birgit Sommer، نويسنده , , Grit Riedel-Herold، نويسنده , , Mark J. Tebbe، نويسنده , , Kenneth J. Thrasher، نويسنده , , Silke Voelkers، نويسنده ,
Abstract :
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.
