Design, synthesis, and biological evaluation studies of novel quinazolinone derivatives as anticonvulsant agents

被引:0
|
作者
Mohamed F. Zayed
Hany E. A. Ahmed
Abdel-Sattar M. Omar
Adel S. Abdelrahim
Khaled El-Adl
机构
[1] College of Pharmacy,Pharmaceutical Chemistry Department
[2] Taibah University,Pharmaceutical Chemistry Department, Faculty of Pharmacy
[3] King AbdulAziz University,Pharmaceutical Chemistry Department, Faculty of Pharmacy
[4] Jazan University,Pharmaceutical Chemistry Department, Faculty of Pharmacy
[5] Al-Azhar University,Organic Chemistry Department, Faculty of Pharmacy
[6] Al-Azhar University,undefined
来源
Medicinal Chemistry Research | 2013年 / 22卷
关键词
Quinazolin-4(3H)-one; Epilepsy; Neurotoxicity; Synthesis; Anticonvulsant;
D O I
暂无
中图分类号
学科分类号
摘要
In view of their expected anticonvulsant activity, some novel derivatives of 6,8-diiodo-2-methyl-3-substituted-quinazolin-4(3H)-ones (4–14) were synthesized, evaluated for their anticonvulsant activity by the maximal electroshock-induced seizure and subcutaneous pentylenetetrazole tests. The neurotoxicity was assessed using rotorod test. All the tested compounds showed considerable anticonvulsant activity in at least one of the anticonvulsant tests. Compounds 5, 6, and 8 proved to be the most potent compounds of this series with relatively low neurotoxicity and low toxicity in the median lethal dose test when compared with the reference drugs. The obtained results showed that the most potent compounds could be useful as a template for future design, optimization, and investigation to produce more active analogs.
引用
收藏
页码:5823 / 5831
页数:8
相关论文
共 50 条
  • [31] Synthesis, biological evaluation, and computational studies of some novel quinazoline derivatives as anticancer agents
    Leila Emami
    Soghra Khabnadideh
    Zahra Faghih
    Farnoosh Farahvasi
    Fatemeh Zonobi
    Saman Zare Gheshlaghi
    Shadi Daili
    Ali Ebrahimi
    Zeinab Faghih
    BMC Chemistry, 16
  • [32] Design, Synthesis, Biological Evaluation, and Molecular Dynamics Studies of Novel Lapatinib Derivatives
    Elkamhawy, Ahmed
    Son, Seohyun
    Lee, Hwa Young
    El-Maghrabey, Mahmoud H.
    El Hamd, Mohamed A.
    Alshammari, Saud O.
    Abdelhameed, Abeer A.
    Alshammari, Qamar A.
    Abdeen, Ahmed
    Ibrahim, Samah F.
    Mahdi, Wael A.
    Alshehri, Sultan
    Alnajjar, Radwan
    Choi, Won Jun
    Al-Karmalawy, Ahmed A.
    Lee, Kyeong
    PHARMACEUTICALS, 2023, 16 (01)
  • [33] Synthesis and Biological Evaluation of Novel Tetrahydroisoquinoline Derivatives as Antitumor Agents
    Wang, Dao-Cai
    Song, Hang
    Yao, Shun
    ASIAN JOURNAL OF CHEMISTRY, 2014, 26 (12) : 3493 - 3495
  • [34] Synthesis and biological evaluation of novel trichodermin derivatives as antifungal agents
    Zheng, Min
    Yao, Ting-Ting
    Xu, Xiao-Jun
    Cheng, Jing-Li
    Zhao, Jin-Hao
    Zhu, Guo-Nian
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2014, 24 (15) : 3565 - 3568
  • [35] Design and synthesis of novel 7-aminoquinazoline derivatives: Antitumor and anticonvulsant activities
    El-Azab, Adel S.
    ElTahir, Kamal E. H.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2012, 22 (05) : 1879 - 1885
  • [36] Synthesis and biological evaluation of novel luteolin derivatives as antibacterial agents
    Lv, Peng-Cheng
    Li, Huan-Qiu
    Xue, Ha-Yu
    Shi, Lei
    Zhu, Hai-Liang
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (02) : 908 - 914
  • [37] Design, Synthesis and Biological Evaluation of Pazopanib Derivatives as Antitumor Agents
    Jia, Yuping
    Zhang, Jian
    Feng, Jinhong
    Xu, Fuming
    Pan, Huili
    Xu, Wenfang
    CHEMICAL BIOLOGY & DRUG DESIGN, 2014, 83 (03) : 306 - 316
  • [38] Synthesis and biological evaluation of novel dibenzofluorene derivatives as anticancer agents
    Banik, Bimal K.
    Mukhopadhyay, Chhanda
    Becker, Frederick F.
    ONCOLOGY LETTERS, 2010, 1 (02) : 309 - 311
  • [39] Synthesis and anticonvulsant activity of novel purine derivatives
    Wang, Shi-Ben
    Jin, Peng
    Li, Fu-Nan
    Quan, Zhe-Shan
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2014, 84 : 574 - 583
  • [40] Synthesis and Biological Activity Evaluation of Some New Coumarin Derivatives as Potent Anticonvulsant and CNS-Depressant Agents
    Al-Humaidi, Jehan Y.
    Nayl, A. A.
    Abdalla, Mohamed M.
    Gomha, Sobhi M.
    POLYCYCLIC AROMATIC COMPOUNDS, 2023, 43 (03) : 2680 - 2689