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Beta 3 agonists. Part 1: evolution from inception to BMS-194449.

W N Washburn1, P M Sher, K M Poss

  • 1Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543, USA. william.washburn@bms.com

Bioorganic & Medicinal Chemistry Letters
|November 21, 2001
PubMed
Summary

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This summary is machine-generated.

Researchers identified novel compounds as beta 3 agonists. Modifications to these molecules enhanced selectivity for the beta 3 receptor, leading to the development of a promising clinical candidate for further study.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology

Background:

  • Beta 3 adrenergic receptors play a role in various physiological processes.
  • Developing selective agonists for beta 3 receptors is a therapeutic goal.

Purpose of the Study:

  • To identify and characterize novel beta 3 adrenergic receptor agonists.
  • To explore structure-activity relationships (SAR) for optimizing beta 3 selectivity.

Main Methods:

  • Screening of the BMS compound collection.
  • Systematic chemical modification and SAR analysis of identified hit compounds.
  • Evaluation of receptor binding and functional activity.

Main Results:

  • 4-hydroxy-3-methylsulfonanilidoethanolamines were identified as full beta 3 agonists.

Related Experiment Videos

  • Substitution on the ethanolamine nitrogen and C(alpha) positions modulated receptor selectivity.
  • Highly selective beta 3 agonists, including 1,1-diarylmethylamines, were discovered.

    • Conclusions:

    • Novel chemical scaffolds targeting beta 3 adrenergic receptors were developed.
    • Structural modifications significantly improved beta 3 selectivity.
    • A potent and selective beta 3 agonist, BMS-194449, was identified as a clinical candidate.