SYNTHESIS, BIOLOGICAL EVALUATION AND MOLECULAR DOCKING OF QUINAZOLINE-4(1H)-ONE DERIVATIVES AS ANTI-INFLAMMATORY AND ANALGESIC AGENTS

被引：0
|
作者：
Mohamed, Mosaad S. [1 ]
Kamel, Mohsen M. [2 ]
Kassem, Emad M. M. [2 ]
Abotaleb, Nageh [1 ]
Khedr, M. [3 ]
Ahmed, Marwa F. [1 ]
机构：
[1] Helwan Univ, Fac Pharm, Helwan, Egypt
[2] Natl Res Ctr, Dept Therapeut Chem, Cairo, Egypt
[3] Cardiff Univ, Welsh Sch Pharm, Cardiff, S Glam, Wales
来源：
ACTA POLONIAE PHARMACEUTICA | 2011年 / 68卷 / 05期
关键词：
quinazolin-4-ones; anti-inflammatory; analgesic; ulcerogenic effect; molecular docking; IN-VITRO; POTENT; INHIBITORS;
D O I：
暂无
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Two series of 2-phenyl-4(3H) quinazolinone derivatives have been synthesized. Most of the tested quinazolinone derivatives showed considerable potent anti-inflammatory and analgesic activity of superior GIT safety profile in experimental rats in comparing to indomethacin as reference drug. Compounds VIa, VIb were the most potent anti-inflammatory in experimental rats in comparing to indomethacin as reference drug. Docking study into COX-2 has been made for derivatives of anti-inflammatory activity.
引用
收藏
页码：665 / 675
页数：11
相关论文
共 50 条
  • [41] Synthesis, Molecular Modelling and Biological Evaluation of Novel Pyrimidine Derivatives as Anti-inflammatory Agents
    Ahmed, Naglaa Mohamed
    Nofal, Shahira
    Awad, Samir Mohamed
    JOURNAL OF PHARMACEUTICAL RESEARCH INTERNATIONAL, 2020, 32 (22) : 49 - 67
  • [42] SYNTHESIS AND BIOLOGICAL EVALUATION OF QUINOLINE DERIVATIVES BEARING THIAZOLIDINONES SCAFFOLDS AS POTENT ANTI-INFLAMMATORY AND ANALGESIC AGENTS
    Gupta, Sujeet Kumar
    Mishra, Ashutosh
    INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY, 2016, 25 (3-4) : 263 - 268
  • [43] Design, Synthesis and Biological Evaluation of 2-Thio Benzoxazole Derivatives as Anti-Inflammatory and Analgesic Agents
    Yin, Di
    Gao, Xiang
    Li, Qing
    Zhao, Nong
    Long, Sheng-jing
    LATIN AMERICAN JOURNAL OF PHARMACY, 2016, 35 (08): : 1701 - 1709
  • [44] Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents
    Biava, Mariangela
    Porretta, Giulio C.
    Poce, Giovanna
    Supino, Sibilla
    Manetti, Fabrizio
    Forli, Stefano
    Botta, Maurizio
    Sautebin, Lidia
    Rossi, Antonietta
    Pergola, Carlo
    Ghelardini, Carla
    Norcini, Monica
    Makovec, Francesco
    Giordani, Antonio
    Anzellotti, Paola
    Cirilli, Roberto
    Ferretti, Rosella
    Gallinella, Bruno
    La Torre, Francesco
    Anzini, Maurizio
    Patrignani, Paola
    BIOORGANIC & MEDICINAL CHEMISTRY, 2008, 16 (17) : 8072 - 8081
  • [45] Synthesis of New Pyrazole Derivatives, Their Anti-Inflammatory and Analgesic Activities, and Molecular Docking Studies
    M. F. El Shehry
    E. F. Ewies
    E. M. Zayed
    Russian Journal of General Chemistry, 2019, 89 : 492 - 498
  • [46] Synthesis of New Pyrazole Derivatives, Their Anti-Inflammatory and Analgesic Activities, and Molecular Docking Studies
    El Shehry, M. F.
    Ewies, E. F.
    Zayed, E. M.
    RUSSIAN JOURNAL OF GENERAL CHEMISTRY, 2019, 89 (03) : 492 - 498
  • [47] Synthesis, characterization, and evaluation of some novel 4(3H)-quinazolinone derivatives as anti-inflammatory and analgesic agents
    Farag, Awatef A.
    Khalifa, Ebtsam M.
    Sadik, Naima A.
    Abbas, Samir Y.
    Al-Sehemi, Abdullah G.
    Ammar, Yousry A.
    MEDICINAL CHEMISTRY RESEARCH, 2013, 22 (01) : 440 - 452
  • [48] Synthesis of New Nicotinic Acid Derivatives and Their Evaluation as Analgesic and Anti-inflammatory Agents
    Khalil, Nadia Abdalla
    Ahmed, Eman Mohamed
    Mohamed, Khaled Omar
    Zaitone, Sawsan Abo-Bakr
    CHEMICAL & PHARMACEUTICAL BULLETIN, 2013, 61 (09) : 933 - 940
  • [49] Synthesis, characterization, and evaluation of some novel 4(3H)-quinazolinone derivatives as anti-inflammatory and analgesic agents
    Awatef A. Farag
    Ebtsam M. Khalifa
    Naima A. Sadik
    Samir Y. Abbas
    Abdullah G. Al-Sehemi
    Yousry A. Ammar
    Medicinal Chemistry Research, 2013, 22 : 440 - 452
  • [50] Synthesis and pharmacological evaluation of pyrazoline derivatives as new anti-inflammatory and analgesic agents
    Amir, Mohammad
    Kumar, Harish
    Khan, Suroor A.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (03) : 918 - 922
12345