Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists

Vu Ma, Anthony W. Bannon, Jamie Baumgartner, Clarence Hale, Faye Hsieh, Christopher Hulme, Kirk Rorrer, John Salon, Carlo van Staden, Paul Tempest

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

Melanin-concentrating hormone (MCH) is a cyclic 19 amino acid orexigenic neuropeptide. The action of MCH on feeding is thought to involve the activation of its respective G protein-coupled receptor MCH-R1. Consequently, antagonists that block MCH regulated MCH-R1 activity may provide a viable approach to the treatment of diet-induced obesity. This communication reports the discovery of a novel MCH-R1 receptor antagonist, the biarylether 7, identified through high throughput screening. The solid-phase synthesis and structure-activity relationship of related analogs is described.

Original languageEnglish (US)
Pages (from-to)5066-5072
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number19
DOIs
StatePublished - Oct 1 2006
Externally publishedYes

Fingerprint

Solid-Phase Synthesis Techniques
Structure-Activity Relationship
Cyclic Amino Acids
G-Protein-Coupled Receptors
Neuropeptides
Nutrition
Obesity
melanin-concentrating hormone
melanin-concentrating hormone receptor
Screening
Diet
Chemical activation
Throughput
Amino Acids
Communication

Keywords

  • Biarylethers
  • MCH-R1 antagonists

ASJC Scopus subject areas

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

Cite this

Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists. / Ma, Vu; Bannon, Anthony W.; Baumgartner, Jamie; Hale, Clarence; Hsieh, Faye; Hulme, Christopher; Rorrer, Kirk; Salon, John; Staden, Carlo van; Tempest, Paul.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 16, No. 19, 01.10.2006, p. 5066-5072.

Research output: Contribution to journalArticle

Ma, Vu ; Bannon, Anthony W. ; Baumgartner, Jamie ; Hale, Clarence ; Hsieh, Faye ; Hulme, Christopher ; Rorrer, Kirk ; Salon, John ; Staden, Carlo van ; Tempest, Paul. / Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists. In: Bioorganic and Medicinal Chemistry Letters. 2006 ; Vol. 16, No. 19. pp. 5066-5072.
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