- 2,4-Thiazolidinediones as potent and selective human β3 agonists
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Methylsulfonamide substituted 2,4-thiazolidinedione 22c is a potent (EC50 = 0.01 μM, IA = 1.19) and selective (more than 110-fold over β1 and β2 agonist activity) β3 agonist. This compound has also been proven to be active and selective in an in vivo mode.
- Hu, Baihua,Ellingboe, John,Gunawan, Iwan,Han, Stella,Largis, Elwood,Li, Zenan,Malamas, Michael,Mulvey, Ruth,Oliphant, Alexander,Sum, Fuk-Wah,Tillett, Jeff,Wong, Victoria
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p. 757 - 760
(2007/10/03)
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- Tricyclic compounds and drug compositions containing the same
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Compounds having a β-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc., represented by a general formula (I) and salts thereof, and a process for producing these, and their intermediates, wherein R represents hydrogen or methyl; R1 represents hydrogen, halogen, hydroxy, benzyloxy, amino, or hydroxymethyl; R2 represents hydrogen, hydroxymethyl, NHR3, SO2 NR4 R4', or nitro; R6 represents hydrogen or lower alkyl; and X represents nitrogen, R9 represents hydrogen, one of R7 and R8 represent hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy.
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