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Synthesis and biological activities of spiroheterocyclic growth hormone secretagogues

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
9
Issue
9
Identifiers
DOI: 10.1016/s0960-894x(99)00183-3
Disciplines
  • Biology

Abstract

Abstract 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.

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