Reduced amide bond neurotensin 8-13 mimetics with potent in vivo activity

D. J. Wustrow, M. D. Davis, H. C. Akunne, A. E. Corbin, J. N. Wiley, L. D. Wise, T. G. Heffner

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Abstract

Appropriately substituted 8-9 (ΨCH2NH) isosteres of neurotensin (NT) 8-13 have been found which are active as NT agonists in vitro and in vivo. SAR studies suggest that preventing amide bond hydrolysis at the 8-9 and 11-12 positions of NT(8-13) mimetics is important for producing compounds with potent activity in vivo. Other simplified replacements for the Arg-Arg portion of NT(8-13) are reported.

Original languageEnglish (US)
Pages (from-to)997-1002
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume5
Issue number9
DOIs
StatePublished - May 4 1995

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ASJC Scopus subject areas

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

Cite this

Wustrow, D. J., Davis, M. D., Akunne, H. C., Corbin, A. E., Wiley, J. N., Wise, L. D., & Heffner, T. G. (1995). Reduced amide bond neurotensin 8-13 mimetics with potent in vivo activity. Bioorganic and Medicinal Chemistry Letters, 5(9), 997-1002. https://doi.org/10.1016/0960-894X(95)00155-M