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

被引：40
|
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
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 06期
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 50 条
  • [1] Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists
    Zhou, Changyou
    Tang, Cheng
    Chang, Eric
    Ge, Min
    Lin, Songnian
    Cline, Eric
    Tan, Carina P.
    Feng, Yue
    Zhou, Yun-Ping
    Eiermann, George J.
    Petrov, Aleksandr
    Salituro, Gino
    Meinke, Peter
    Mosley, Ralph
    Akiyama, Taro E.
    Einstein, Monica
    Kumar, Sanjeev
    Berger, Joel
    Howard, Andrew D.
    Thornberry, Nancy
    Mills, Sander G.
    Yang, Lihu
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (03) : 1298 - 1301
  • [2] Synthesis and biological activity of [[(heterocycloamino)alkoxy] benzyl]-2,4-thiazolidinediones as PPARγ agonists
    Raok Jeon
    Yoon-Jung Kim
    Yejin Cheon
    Jae-Ha Ryu
    [J]. Archives of Pharmacal Research, 2006, 29
  • [3] Synthesis and biological activity of [[(heterocycloamino)alkoxy] benzyl]-2,4-thiazolidinediones as PPARγ agonists
    Jeon, R
    Kim, YJ
    Cheon, Y
    Ryu, JH
    [J]. ARCHIVES OF PHARMACAL RESEARCH, 2006, 29 (05) : 394 - 399
  • [4] Synthesis and antihyperglycemic activity of 2,4-thiazolidinediones
    Chavan, Ameya A.
    Pai, Nandini R.
    [J]. INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY, 2007, 17 (01) : 45 - 48
  • [5] Chemistry and Applications of Functionalized 2,4-Thiazolidinediones
    Ibrahim, Ayman M. M.
    Shoman, Mai E. E.
    Mohamed, Mamdouh F. A.
    Hayallah, Alaa M. M.
    Abuo-Rahma, Gamal El-Din A.
    [J]. EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, 2023, 26 (19)
  • [6] A new series of 2,4-thiazolidinediones endowed with potent aldose reductase inhibitory activity
    Sever, Belgin
    Altintop, Mehlika Dilek
    Demir, Yeliz
    Turkes, Cuneyt
    Ozbas, Kaan
    Ciftci, Gulsen Akalin
    Beydemir, Sukru
    Ozdemir, Ahmet
    [J]. OPEN CHEMISTRY, 2021, 19 (01): : 347 - 357
  • [7] [[OMEGA-(HETEROCYCLYLAMINO)ALKOXY]BENZYL]-2,4-THIAZOLIDINEDIONES AS POTENT ANTIHYPERGLYCEMIC AGENTS
    CANTELLO, BCC
    CAWTHORNE, MA
    COTTAM, GP
    DUFF, PT
    HAIGH, D
    KINDLEY, RM
    LISTER, CA
    SMITH, SA
    THURLBY, PL
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (23) : 3977 - 3985
  • [8] 5-ARALKYLIDENE-3-ISOBUTYL-2,4-THIAZOLIDINEDIONES
    LO, CP
    SHROPSHIRE, EY
    CROXALL, WJ
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1953, 75 (19) : 4845 - 4846
  • [9] Recent Pharmacological Developments on Rhodanines and 2,4-Thiazolidinediones
    Bhatti, Ravinder Singh
    Shah, Sakshi
    Suresh
    Krishan, Pawan
    Sandhu, Jagir S.
    [J]. INTERNATIONAL JOURNAL OF MEDICINAL CHEMISTRY, 2013, 2013
  • [10] Insulinotropic activity of chromonyl-2,4-thiazolidinediones
    Verspohl, Eugen J.
    Bozdag-Dundar, Oya
    Kaup, Rebecca M.
    Bauer, Katrin
    Ertan, Rahmiye
    [J]. MEDICINAL CHEMISTRY RESEARCH, 2009, 18 (08) : 665 - 670
12345