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

Feng Hong, Javid Zaidi, Bernadette Cusack, Elliott Richelson

Research output: Contribution to journalArticle

33 Citations (Scopus)

Abstract

Novel neurotensin (NT) (8-13) (Arg 8-Arg 9-Pro 10-Tyr 11-Ile 12-Leu 13) 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

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neurotensin (8-13)
Neurotensin Receptors
Functional groups
Rats

ASJC Scopus subject areas

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

Cite this

Synthesis and biological studies of novel neurotensin(8-13) mimetics. / Hong, Feng; Zaidi, Javid; Cusack, Bernadette; Richelson, Elliott.

In: Bioorganic and Medicinal Chemistry, Vol. 10, No. 12, 01.12.2002, p. 3849-3858.

Research output: Contribution to journalArticle

Hong, Feng ; Zaidi, Javid ; Cusack, Bernadette ; Richelson, Elliott. / Synthesis and biological studies of novel neurotensin(8-13) mimetics. In: Bioorganic and Medicinal Chemistry. 2002 ; Vol. 10, No. 12. pp. 3849-3858.
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