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 Scopus citations

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

Keywords

  • Biarylethers
  • MCH-R1 antagonists

ASJC Scopus subject areas

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

Fingerprint Dive into the research topics of 'Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists'. Together they form a unique fingerprint.

  • Cite this