2,4-Thiazolidinediones as potent and selective human beta3 agonists.
Methylsulfonamide substituted 2,4-thiazolidinedione 22c is a potent (EC50=0.01 microM, IA=1.19) and selective (more than 110-fold over beta1 and beta2 agonist activity) beta3 agonist. This compound has also been proven to be active and selective in an in vivo mode.
Chemical Sciences, Wyeth-Ayerst Research, Pearl River, NY 10965, USA. hub@war.wyeth.com
B
B
Hu
J
J
Ellingboe
I
I
Gunawan
S
S
Han
E
E
Largis
Z
Z
Li
M
M
Malamas
R
R
Mulvey
A
A
Oliphant
F W
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Sum
J
J
Tillett
V
V
Wong
D058667:Adrenergic beta-3 Receptor Agonists; D000818:Animals; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D004195:Disease Models, Animal; D006801:Humans; D051379:Mice; D018345:Mice, Knockout; D008822:Mice, Transgenic; D009765:Obesity / Q000188:drug therapy; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D045162:Thiazolidinediones
D058667:Adrenergic beta-3 Receptor Agonists; D013844:Thiazoles; D045162:Thiazolidinediones; C089946:2,4-thiazolidinedione