Synthesis and biological studies of novel neurotensin(8-13) mimetics

Feng Hong, Javid Zaidi, Bernadette Cusack, Elliott Richelson

Research output: Contribution to journalArticle

33 Scopus citations

Abstract

Novel neurotensin (NT) (8-13) (Arg8-Arg9-Pro10-Tyr11-Ile 12-Leu13) mimetics 3, 4 were designed by adopting all intrinsic functional groups of the native neurotensin(8-13) and using a substituted indole as a template to mimic the pharmacophore of NT(8-13). Biological studies at subtype 1 of the NT receptor showed that 3 has a 55 and 580 nM binding affinity at rat and human neurotensin receptors, respectively. As a comparison, compounds 5 and 6 were also synthesized. The binding difference between 3, 4 and 5, 6 argues the importance of the carboxylic group in achieving higher potency NT(8-13) mimetics.

Original languageEnglish (US)
Pages (from-to)3849-3858
Number of pages10
JournalBioorganic and Medicinal Chemistry
Volume10
Issue number12
DOIs
StatePublished - Dec 1 2002

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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