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Structure activity studies of the serine-AIB dipeptide domain in 2,3-dihydroisothiazole based growth hormone secretagogues |
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| Authors: | 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 |
| Institution: | aLilly Forschung GmbH, Division of Eli Lilly Research Laboratories, Essener Bogen 7, 22419 Hamburg, Germany bLilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA |
| 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. |
| Keywords: | Growth hormone Growth hormone secretagogue |
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