DESIGN, SYNTHESIS AND VIRTUAL SCREENING OF CERTAIN 2-PYRAZOLIN-5-ONE AND PYRAZOLIDINE-3, 5-DIONE DERIVATIVES AS POTENTIAL PPAR gamma AGONISTS

被引：4
|
作者：
Ismaila, Mohamed A. H. [1 ]
El Ella, Dalal A. Abou [1 ]
Abouzid, Khaled A. M. [1 ]
Jaballah, Maiy [1 ]
机构：
[1] Ain Shams Univ, Fac Pharm, Dept Pharmaceut Chem, El Khalifa ElMaamoon St, Cairo 11566, Egypt
来源：
INTERNATIONAL JOURNAL OF PHARMACEUTICAL SCIENCES AND RESEARCH | 2012年 / 3卷 / 10期
关键词：
PPAR gamma; Pyrazolin-5-one; Pyrazolidine-3; 5-dione; Design;
D O I：
10.13040/IJPSR.0975-8232.3(10).3746-57
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
In the quest for novel PPAR gamma agonists as putative drugs for the treatment of type 2 diabetes, a new series of 2-pyrazolin-5-one and pyrazolidine-3, 5-dione derivatives, were designed and synthesized, as analogues to the antidiabetic thiazolidinedione agents (TZDs). Extensive molecular modeling studies for the designed molecules were performed; including their compare-fit studies on the generated and validated PPAR gamma agonist's hypothesis and their molecular docking on the binding sites of the 3D structure of the PPAR gamma receptors.
引用
收藏
页码：3746 / 3757
页数：12
相关论文
共 50 条
  • [1] PYRAZOLINE-5-ONE AND PYRAZOLIDINE-3,5-DIONE DERIVATIVES WITH ANTIPHLOGISTIC AND ANALGESIC ACTIVITY
    NARDI, D
    MASSARANI, E
    MAGISTRETTI, MJ
    [J]. ARZNEIMITTEL-FORSCHUNG, 1969, 19 (10): : 1721 - +
  • [2] Design and Synthesis of 1-Benzylidene-pyrazolidine-3, 5-Dione Derivatives
    Li, Xing
    Yao, Zhiyi
    [J]. 2015 4TH INTERNATIONAL CONFERENCE ON ENERGY AND ENVIRONMENTAL PROTECTION (ICEEP 2015), 2015, : 1736 - 1742
  • [3] Pyrazolidine-3,5-dione derivatives as potent non-steroidal agonists of farnesoid X receptor: Virtual screening, synthesis, and biological evaluation
    Deng, Guanghui
    Li, Weihua
    Shen, Jianhua
    Jiang, Hualiang
    Chen, Kaixian
    Liu, Hong
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (20) : 5497 - 5502
  • [4] SYNTHESIS OF SOME 2-PYRAZOLIN-5-ONE DERIVATIVES STRUCTURALLY RELATED TO CERTAIN ANALGESIS AND ANTIPYRETIC DRUGS
    METWALLY, MA
    FADDA, AA
    HASSAN, HM
    AFSAH, E
    [J]. ORGANIC PREPARATIONS AND PROCEDURES INTERNATIONAL, 1985, 17 (03) : 198 - 203
  • [5] Design and synthesis of fluorinated pyrazolidine-3,5-dione derivatives as potential P2Y12 receptor PET tracers
    Steen, E. Johanna
    Van der Wildt, Berend
    Zarzycka, Barbara
    Beaino, Wissam
    Vugts, Danielle
    De Esch, Iwan
    Windhorst, Albert
    [J]. NUCLEAR MEDICINE AND BIOLOGY, 2023, 126 : S144 - S145
  • [6] SYNTHESIS AND ANTIMICROBIAL EVALUATION OF 4-BENZYLIDENE-PYRAZOLIDINE-3, 5-DIONE DERIVATIVES
    Kumar, Harish
    Jain, Sandeep
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICAL SCIENCES AND RESEARCH, 2013, 4 (01): : 453 - 457
  • [7] SYNTHESIS AND FUNGITOXICITY OF COBALT(II) COMPLEXES WITH 2-PYRAZOLIN-5-ONE DERIVATIVES
    NAYAK, A
    DAS, NB
    MAHAPATRA, BB
    MITTRA, AS
    [J]. JOURNAL OF THE INDIAN CHEMICAL SOCIETY, 1981, 58 (04) : 347 - 349
  • [8] SYNTHESIS, CHARACTERIZATION AND PHARMACOLOGICAL ACTIVITIES OF PYRIMIDINE DERIVATIVES CONTAINING 2-PYRAZOLIN-5-ONE
    Youssef, Mohamed Salah K.
    Abeed, Ahmed Abdou O.
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICAL SCIENCES AND RESEARCH, 2014, 5 (05): : 1705 - +
  • [9] PREPARATION OF 3-SUBSTITUTED AND 3,4-SUBSTITUTED DERIVATIVES OF 2-PYRAZOLIN-5-ONE
    KONRAD, J
    JEZO, I
    [J]. CHEMICKE ZVESTI, 1980, 34 (01): : 125 - 128
  • [10] SYNTHESIS OF N-ISONICOTINYL-3-METHYL-4-(SUBSTITUTED HYDRAZONO)-2-PYRAZOLIN-5-ONE
    SINGH, CP
    OJHA, AC
    [J]. JOURNAL OF THE INDIAN CHEMICAL SOCIETY, 1980, 57 (12) : 1172 - 1173
12345