2,4-thiazolidinediones as potent and selective human β3 agonists

被引:41
作者
Hu, BH [1 ]
Ellingboe, J
Gunawan, I
Han, S
Largis, E
Li, ZA
Malamas, M
Mulvey, R
Oliphant, A
Sum, FW
Tillett, J
Wong, V
机构
[1] Wyeth Ayerst Res, Chem Sci, Pearl River, NY 10965 USA
[2] Wyeth Ayerst Res, Cardiovasc Metab Dis Res, Pearl River, NY 10965 USA
关键词
D O I
10.1016/S0960-894X(01)00063-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Methylsulfonamide substituted 2,4-thiazolidinedione 22c is a potent (EC50 = 0.01 muM, IA = 1.19) and selective (more than 110-fold over beta (1) and beta (2) agonist activity) beta (3) agonist. This compound has also been proven to be active and selective in an in vivo mode. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:757 / 760
页数:4
相关论文
共 23 条
[1]  
Alvarez SG, 1997, SYNTHESIS-STUTTGART, P413
[2]   A simplified template approach towards the synthesis of a potent beta-3 adrenoceptor agonist at the human receptor [J].
Beeley, LJ ;
Berge, JM ;
Chapman, H ;
Dean, DK ;
Kelly, J ;
Lowden, K ;
Kotecha, NR ;
Morgan, HKA ;
Rami, HK ;
Thompson, M ;
Vong, AKK ;
Ward, RW .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1997, 7 (02) :219-224
[3]  
BELL MG, 1998, Patent No. 708621
[4]   DISODIUM (R,R)-5-[2-[[2-(3-CHLOROPHENYL)-2-HYDROXYETHYL]AMINO]PROPYL]-1,3-BENZODIOXOLE-2,2-DICARBOXYLATE (CL 316,243) - A POTENT BETA-ADRENERGIC AGONIST VIRTUALLY SPECIFIC FOR BETA-3 RECEPTORS - A PROMISING ANTIDIABETIC AND ANTIOBESITY AGENT [J].
BLOOM, JD ;
DUTIA, MD ;
JOHNSON, BD ;
WISSNER, A ;
BURNS, MG ;
LARGIS, EE ;
DOLAN, JA ;
CLAUS, TH .
JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (16) :3081-3084
[5]  
Dow R L, 1997, Expert Opin Investig Drugs, V6, P1811, DOI 10.1517/13543784.6.12.1811
[6]  
GUY A, 1992, SYNLETT, P821
[7]  
HU B, 2000, UNPUB
[8]  
HU BL, UNPUB
[9]  
Katsilambros, 2000, Eur J Intern Med, V11, P65, DOI 10.1016/S0953-6205(00)00063-7
[10]   Pharmacological treatment of obesity: Therapeutic strategies [J].
Kordik, CP ;
Reitz, AB .
JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (02) :181-201