2. Academic Validation
  3. Potent and selective, sulfamide-based human beta 3-adrenergic receptor agonists

Potent and selective, sulfamide-based human beta 3-adrenergic receptor agonists

  • Bioorg Med Chem Lett. 2004 Jun 21;14(12):3235-40. doi: 10.1016/j.bmcl.2004.03.089.
Robert L Dow 1,  Ernest S Paight,  Steven R Schneider,  John R Hadcock,  Diane M Hargrove,  Kelly A Martin,  Tristan S Maurer,  Nancy A Nardone,  David A Tess,  Paul DaSilva-Jardine
Affiliations

Affiliation

  • 1 Cardiovascular and Metabolic Diseases, Pfizer Global Research and Development, Groton, CT 06340, USA. robert_l_dow@groton.pfizer.com
PMID: 15149682 DOI: 10.1016/j.bmcl.2004.03.089
Abstract

A series of sulfamide-based analogs related to L-796568 were prepared and evaluated for their biological activity at the human beta(3)-adrenergic receptor (AR). This modification allows for a significant reduction in molecular weight, while maintaining single-digit nanomolar potencies at the beta(3)-AR and high selectivities versus the beta(2)- or beta(3)-AR.

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