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Related Experiment Videos

Biaryl amide glucagon receptor antagonists.

Ravi Kurukulasuriya1, Bryan K Sorensen, James T Link

  • 1Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA. ravi.kurukulasuriya@abbott.com

Bioorganic & Medicinal Chemistry Letters
|April 15, 2004
PubMed
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New biaryl amides act as potent human glucagon receptor antagonists. A specific benzofuran compound effectively blocked glucagon

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Endocrinology

Background:

  • Glucagon receptor antagonists are potential therapeutic agents for metabolic diseases.
  • Previous research identified urea derivatives with potential biological activity.

Purpose of the Study:

  • To synthesize and evaluate novel biaryl amides as human glucagon receptor antagonists.
  • To assess the in vivo efficacy of a lead compound in a preclinical model.

Main Methods:

  • Synthesis of biaryl amides based on known urea scaffolds.
  • In vitro evaluation of antagonist potency at the human glucagon receptor.
  • In vivo administration of the benzofuran analogue 6i in Sprague-Dawley rats.

Main Results:

Related Experiment Videos

  • Several biaryl amides demonstrated potent antagonism of the human glucagon receptor.
  • The benzofuran analogue 6i significantly blocked the physiological effects of exogenous glucagon in rats.

Conclusions:

  • Biaryl amides represent a promising class of human glucagon receptor antagonists.
  • Compound 6i shows potential for further development as a therapeutic agent for conditions involving elevated glucagon levels.