Potent and selective, sulfamide-based human beta 3-adrenergic receptor agonists |
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| Authors: | Dow Robert L Paight Ernest S Schneider Steven R Hadcock John R Hargrove Diane M Martin Kelly A Maurer Tristan S Nardone Nancy A Tess David A DaSilva-Jardine Paul |
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| Institution: | Cardiovascular and Metabolic Diseases, Pfizer Global Research and Development, Groton, CT 06340, USA. robert_l_dow@groton.pfizer.com |
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| 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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