Design, synthesis and evaluation of peroxisome proliferator-activated receptor α/γ dual agonists for the treatment of type 2 diabetes

被引：0
|
作者：
Das, Saibal Kumar [1 ]
Abbineni, Chandrasekhar [1 ]
Rao, Krovvidi Venkata Lakshmi Narasimha [1 ]
Iqbal, Javed [1 ]
Babu, Ravi Krishna [1 ]
Chakrabarti, Ranjan [1 ]
机构：
[1] Dr Reddys Labs Ltd, Metab Disorders Grp, Discovery Res, Hyderabad 500049, Andhra Pradesh, India
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2007年 / 4卷 / 01期
关键词：
PPAR; diabetes; synthesis; ethyl 3-(4-aminophenyl)-2-ethoxypropionate; dyslipidemia and plasma glucose;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The design, synthesis and evaluation of several dual PPAR alpha/gamma agonists with three different heterocycles, viz. pyrazolo[4,3-d]pyrimidin-7-one, quinazolin-4-one and benzo[e][1,3]oxazine-4-one for the treatment of type 2 diabetes and associated dyslipidemia are described. Among them, compound 5cb was found to possess a potent dual PPAR alpha/gamma agonist property. It significantly reversed diabetic hyperglycemia while improving overall lipid homeostasis in preclinical animal models.
引用
收藏
页码：27 / 32
页数：6
相关论文
共 50 条
  • [41] The Renoprotective Actions of Peroxisome Proliferator-Activated Receptors Agonists in Diabetes
    Thomas, M. C.
    Jandeleit-Dahm, K. A.
    Tikellis, C.
    PPAR RESEARCH, 2012, 2012
  • [42] Synthesis and Structure-Activity Relationships of 2-Aminoacetamide Derivatives as Peroxisome Proliferator-Activated Receptor α/γ Dual Agonists
    Shibata, Yoshihiro
    Kagechika, Katsuji
    Ota, Masahiro
    Yamaguchi, Mitsuhiro
    Setoguchi, Masaki
    Kubo, Hideo
    Chiba, Kiyoshi
    Takano, Hiromichi
    Akiyama, Chiyuki
    Ono, Mayumi
    Nishi, Mina
    Usui, Hiroyuki
    CHEMICAL & PHARMACEUTICAL BULLETIN, 2015, 63 (08) : 591 - 602
  • [43] Effects of the dual peroxisome proliferator-activated receptor activator aleglitazar in patients with Type 2 Diabetes mellitus or prediabetes
    Erdmann, Erland
    Califf, Robert
    Gerstein, Hertzel C.
    Malmberg, Klas
    Ruilope, Luis
    Schwartz, Gregory G.
    Wedel, Hans
    Volz, Dietmar
    Ditmarsch, Marc
    Svensson, Anders
    Bengus, Monica
    AMERICAN HEART JOURNAL, 2015, 170 (01) : 117 - 122
  • [44] The Agonists of Peroxisome Proliferator-Activated Receptor-γ for Liver Fibrosis
    Li, Jingjing
    Guo, Chuanyong
    Wu, Jianye
    DRUG DESIGN DEVELOPMENT AND THERAPY, 2021, 15 : 2619 - 2628
  • [45] Peroxisome proliferator-activated receptor gamma agonists in renal disease
    Iglesias, Pedro
    Diez, Juan J.
    EUROPEAN JOURNAL OF ENDOCRINOLOGY, 2006, 154 (05) : 613 - 621
  • [46] Rhodanine derivatives as novel peroxisome proliferator-activated receptor γ agonists
    Qing LIU
    ActaPharmacologicaSinica, 2007, (12) : 2033 - 2039
  • [47] Rhodanine derivatives as novel peroxisome proliferator-activated receptor γ agonists
    Qing Liu
    Yue-yun Zhang
    Hui-li Lu
    Qun-yi Li
    Cai-hong Zhou
    Ming-wei Wang
    Acta Pharmacologica Sinica, 2007, 28 : 2033 - 2039
  • [48] Two homoisoflavonoids act as peroxisome proliferator-activated receptor agonists
    Lin, Hsiang-Ru
    MEDICINAL CHEMISTRY RESEARCH, 2015, 24 (07) : 2898 - 2905
  • [49] Rhodanine derivatives as novel peroxisome proliferator-activated receptor γ agonists
    Liu, Qing
    Zhang, Yue-yun
    Lu, Hui-li
    Li, Qun-yi
    Zhou, Cai-hong
    Wang, Ming-wei
    ACTA PHARMACOLOGICA SINICA, 2007, 28 (12) : 2033 - 2039
  • [50] Peroxisome proliferator-activated receptor α agonists as therapy for autoimmune disease
    Lovett-Racke, AE
    Hussain, RZ
    Northrop, S
    Choy, J
    Rocchini, A
    Matthes, L
    Chavis, JA
    Diab, A
    Drew, PD
    Racke, MK
    JOURNAL OF IMMUNOLOGY, 2004, 172 (09): : 5790 - 5798
12345