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
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
  • [41] Synthesis and In Vitro Cytotoxicity Evaluation of Phenanthrene Linked 2,4-Thiazolidinediones as Potential Anticancer Agents
    Yadav, Upasana
    Vanjari, Yogesh
    Laxmikeshav, Kritika
    Tokala, Ramya
    Niggula, Praveen K.
    Kumar, Manoj
    Talla, Venu
    Kamal, Ahmed
    Shankaraiah, Nagula
    [J]. ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY, 2021, 21 (09) : 1127 - 1140
  • [42] Synthesis, biological evaluation and molecular docking studies of novel 3,5-disubstituted 2,4-thiazolidinediones derivatives
    Srivastava, Alok Ranjan
    Bhatia, Rohit
    Chawla, Pooja
    [J]. BIOORGANIC CHEMISTRY, 2019, 89
  • [43] Synthesis and antihyperglycemic evaluation of new 2,4-thiazolidinediones having biodynamic aryl sulfonylurea moieties
    Jawale, Dhanaji V.
    Pratap, Umesh R.
    Rahuja, Neha
    Srivastava, Arvind K.
    Mane, Ramrao A.
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2012, 22 (01) : 436 - 439
  • [44] SYNTHESIS OF LONG-CHAIN SUBSTITUTED 2-IMINO-4-THIAZOLIDINONES AND 2,4-THIAZOLIDINEDIONES
    MUKARRAM, M
    AHMAD, I
    FAROOQI, JA
    AHMAD, M
    [J]. FETTE SEIFEN ANSTRICHMITTEL, 1986, 88 (06): : 224 - 226
  • [45] QSAR analysis of 5-arylidene-2,4-thiazolidinediones as aldose reductase inhibitors
    Sambasivarao, S. V.
    Soni, L. K.
    Gupta, A. K.
    Kaskhedikar, S. G.
    [J]. JOURNAL OF PHARMACY AND PHARMACOLOGY, 2005, 57 : S34 - S35
  • [46] QSAR study of 5-arylidene-2,4-thiazolidinediones as aldose reductase inhibitors
    Love Kumar Soni
    Arun Kumar Gupta
    S. G. Kaskhedikar
    [J]. Medicinal Chemistry Research, 2008, 17 : 258 - 266
  • [47] SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME 5-(1-METHYLALKYLIDENE)-2,4-THIAZOLIDINEDIONES
    BROWN, FC
    BRADSHER, CK
    CHILTON, SW
    [J]. JOURNAL OF ORGANIC CHEMISTRY, 1956, 21 (11): : 1269 - 1271
  • [48] 4-THIAZOLIDINONES AND 2,4-THIAZOLIDINEDIONES FROM ALPHA-MERCAPTOPROPIONIC ACID AND CARBODIIMIDES
    MONFORTE, P
    FENECH, G
    BASILE, M
    FICARRA, P
    SILVESTRO, A
    [J]. JOURNAL OF HETEROCYCLIC CHEMISTRY, 1979, 16 (02) : 341 - 345
  • [49] Antimicrobial screening of new 5-(chromene-3-yl) methylene-2,4-thiazolidinediones
    Nastasa, Cristina
    Duma, Mihaela
    Tiperciuc, Brindusa
    Oniga, Ovidiu
    [J]. BANGLADESH JOURNAL OF PHARMACOLOGY, 2015, 10 (03)
  • [50] RECYCLIZATION REACTIONS .25. RECYCLIZATIONS OF "3-ACYLMETHYL-2,4-THIAZOLIDINEDIONES UNDER THE EFFECT OF NUCLEOPHILS
    SHVAIKA, OP
    KOROTKIKH, NI
    CHERVINSKII, AY
    ARTEMOV, VN
    [J]. ZHURNAL ORGANICHESKOI KHIMII, 1983, 19 (08): : 1728 - 1739