2. Academic Validation
  3. Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor

Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor

  • Bioorg Med Chem Lett. 1998 May 5;8(9):1101-6. doi: 10.1016/s0960-894x(98)00169-3.
A E Weber 1,  R J Mathvink,  L Perkins,  J E Hutchins,  M R Candelore,  L Tota,  C D Strader,  M J Wyvratt,  M H Fisher
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, USA.
PMID: 9871716 DOI: 10.1016/s0960-894x(98)00169-3
Abstract

A cloned human beta 3 Adrenergic Receptor assay was used to identify phenoxypropanolamine agonist 1. SAR studies led to the identification of benzenesulfonamide derivative 20, a 6.3 nM beta 3 agonist which shows 30-fold selectivity for beta 3 agonist activity over beta 1 and beta 2 receptor binding. Further refinement of this lead provided 4-bromo derivative 39, a subnanomolar agonist with 660-fold and 230-fold selectivity over beta 1 and beta 2, respectively.

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