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
  • [21] Design, Synthesis, Molecular docking, and biological evaluation of novel 2,3-diaryl-1,3-thiazolidine-4-one derivatives as potential anti-inflammatory and cytotoxic agents
    Mekhlef, Yosra O.
    AboulMagd, Asmaa M.
    Gouda, Ahmed M.
    BIOORGANIC CHEMISTRY, 2023, 133
  • [22] Design, synthesis, biological evaluation, and molecular docking study on triazine based derivatives as anti-inflammatory agents
    Asadi, Parvin
    Alvani, Mohsen
    Hajhashemi, Valiollah
    Rostami, Mahboubeh
    Khodarahmi, Ghadamali
    JOURNAL OF MOLECULAR STRUCTURE, 2021, 1243
  • [23] Molecular docking and synthesis of caffeic acid analogous and its anti-inflammatory, analgesic and ulcerogenic studies
    Al-Ostoot, Fares Hezam
    Zabiulla
    Grisha, S.
    Mohammed, Yasser Hussein Eissa
    Vivek, H. K.
    Khanum, Shaukath Ara
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021, 33
  • [24] 4-Aminoantipyrine Analogs as Anti-inflammatory and Antioxidant agents: Synthesis, Biological Evaluation and Molecular Docking Studies
    Yasar, Qazi
    Zaheer, Zahid
    INTERNATIONAL JOURNAL OF PHARMACEUTICAL INVESTIGATION, 2021, 11 (01) : 14 - 22
  • [25] Synthesis, biological evaluation and molecular docking study of some new 4-aminosalicylic acid derivatives as anti-inflammatory and antimycobacterial agents
    Qahtan, Maha Q. M.
    Bakhite, Etify A.
    Kumari, Jyothi
    Sayed, Ahmed M.
    Kandeel, Mahmoud
    Sriram, Dharmarajan
    Abdu-Allah, Hajjaj H. M.
    BIOORGANIC CHEMISTRY, 2023, 132
  • [26] Synthesis, biological evaluation and molecular docking studies of N-acylheteroaryl hydrazone derivatives as antioxidant and anti-inflammatory agents
    Mahajan, Pravin S.
    Nikam, Mukesh D.
    Khedkar, Vijay M.
    Jha, Prakash C.
    Sarkar, Dhiman
    Gill, Charansingh H.
    RESEARCH ON CHEMICAL INTERMEDIATES, 2016, 42 (03) : 2707 - 2729
  • [27] Synthesis, analgesic and anti-inflammatory evaluation of some new 3H-quinazolin-4-one derivatives
    Alafeefy, Ahmed M.
    Kadi, Adnan A.
    El-Azab, Adel S.
    Abdel-Hamide, Sami G.
    Daba, Mohamad-Hesham Y.
    ARCHIV DER PHARMAZIE, 2008, 341 (06) : 377 - 385
  • [28] Design, synthesis, anti-inflammatory, analgesic screening, and molecular docking of some novel 2-pyridyl (3H)-quinazolin-4-one derivatives
    Eweas, Ahmad F.
    El-Nezhawy, Ahmed O. H.
    Baiuomy, Ayman R.
    Awad, Mohamed M.
    MEDICINAL CHEMISTRY RESEARCH, 2013, 22 (02) : 1011 - 1020
  • [29] 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
  • [30] Synthesis and Biological Evaluation of Novel Pyrazole Derivatives as Anti-Inflammatory Antimicrobial Agents
    Bekhit, Adnan A.
    Ashour, Hayam M. A.
    Bekhit, Alaa El-Din A.
    Bekhit, Salma A.
    MEDICINAL CHEMISTRY, 2009, 5 (02) : 103 - 117