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Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor. 1998
A E Weber, and
R J Mathvink, and
L Perkins, and
J E Hutchins, and
M R Candelore, and
L Tota, and
C D Strader, and
M J Wyvratt, and
M H Fisher
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, USA.
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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A E Weber, and
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L Perkins, and
J E Hutchins, and
M R Candelore, and
L Tota, and
C D Strader, and
M J Wyvratt, and
M H Fisher
November 1998,
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M J Wyvratt, and
M H Fisher
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M R Candelore, and
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Bioorganic & medicinal chemistry letters,
A E Weber, and
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M J Wyvratt, and
M H Fisher
November 2006,
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A E Weber, and
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M R Candelore, and
L Tota, and
C D Strader, and
M J Wyvratt, and
M H Fisher
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The Journal of pharmacology and experimental therapeutics,
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R J Mathvink, and
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M R Candelore, and
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M H Fisher
December 2001,
Bioorganic & medicinal chemistry letters,
A E Weber, and
R J Mathvink, and
L Perkins, and
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M R Candelore, and
L Tota, and
C D Strader, and
M J Wyvratt, and
M H Fisher
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Bioorganic & medicinal chemistry letters,
A E Weber, and
R J Mathvink, and
L Perkins, and
J E Hutchins, and
M R Candelore, and
L Tota, and
C D Strader, and
M J Wyvratt, and
M H Fisher
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Journal of medicinal chemistry,
A E Weber, and
R J Mathvink, and
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M R Candelore, and
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M H Fisher
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