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

被引:31
|
作者
Zayed, Mohamed F. [1 ,4 ]
Ahmed, Hany E. A. [1 ,5 ]
Omar, Abdel-Sattar M. [2 ,4 ]
Abdelrahim, Adel S. [3 ,4 ]
El-Adl, Khaled [4 ]
机构
[1] Taibah Univ, Coll Pharm, Dept Pharmaceut Chem, Al Madinah Al Munawarah, Saudi Arabia
[2] King Abdulaziz Univ, Fac Pharm, Dept Pharmaceut Chem, Jeddah 21413, Saudi Arabia
[3] Jazan Univ, Dept Pharmaceut Chem, Fac Pharm, Jazan, Saudi Arabia
[4] Al Azhar Univ, Fac Pharm, Dept Pharmaceut Chem, Cairo, Egypt
[5] Al Azhar Univ, Fac Pharm, Dept Organ Chem, Cairo, Egypt
关键词
Quinazolin-4(3H)-one; Epilepsy; Neurotoxicity; Synthesis; Anticonvulsant;
D O I
10.1007/s00044-013-0569-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
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:9
相关论文
共 50 条
  • [1] Design, synthesis, and biological evaluation studies of novel quinazolinone derivatives as anticonvulsant agents
    Mohamed F. Zayed
    Hany E. A. Ahmed
    Abdel-Sattar M. Omar
    Adel S. Abdelrahim
    Khaled El-Adl
    Medicinal Chemistry Research, 2013, 22 : 5823 - 5831
  • [2] Novel quinazolinone derivatives as anticancer agents: Design, synthesis, biological evaluation and computational studies
    Ataollahi, Elaheh
    Behrouz, Marzieh
    Mardaneh, Pegah
    Emami, Mina
    Zare, Somayeh
    Zafarian, Hamidreza
    Khabnadideh, Soghra
    Emami, Leila
    JOURNAL OF MOLECULAR STRUCTURE, 2024, 1295
  • [3] Synthesis and biological evaluation studies of novel quinazolinone derivatives as antibacterial and anti-inflammatory agents
    Zayed, Mohamed F.
    Hassan, Memy H.
    SAUDI PHARMACEUTICAL JOURNAL, 2014, 22 (02) : 157 - 162
  • [4] Design, synthesis and biological evaluation of new quinazolinone derivatives as potent antimicrobial agents
    Nanduri, Srinivas
    Gatadi, Srikanth
    Yeddanapudi, Madhavi
    Chopra, Sidharth
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2017, 254
  • [5] Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives as Potential Anticonvulsant Agents
    Liu, Da-Chuan
    Zhang, Hong-Jian
    Jin, Chun-Mei
    Quan, Zhe-Shan
    MOLECULES, 2016, 21 (02)
  • [6] Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives as Potential Anticonvulsant Agents
    Liu, Da-Chuan
    Zhang, Hong-Jian
    Jin, Chun-Mei
    Quan, Zhe-Shan
    MOLECULES, 2016, 21 (03)
  • [7] SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL IMIDAZOLE DERIVATIVES AS POTENT ANTICONVULSANT AGENTS
    Mohammad, Noor
    Tabassum, Ruby
    Kishor, Brajnandan
    Srivastava, Neha
    Yogi, Bhumika
    Sinha, Anshuman
    Gupta, Sujeet K.
    INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY, 2017, 27 (02) : 137 - 142
  • [8] Synthesis and biological evaluation of some novel quinoxaline derivatives as anticonvulsant agents
    Elhelby, Abdelghany Aly
    Ayyad, Rezk Rezk
    Zayed, Mohamed Fathalla
    ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH, 2011, 61 (07): : 379 - 381
  • [9] Design, synthesis and biological evaluation of novel spiro-quinazolinone derivatives as chitin synthase inhibitors and antifungal agents
    Du, Chuanbiao
    Yang, Xinlong
    Long, Yan
    Lang, Xueqing
    Liu, Lige
    Xu, Yajie
    Wu, Hu
    Chu, Yiwen
    Hu, Xiaolei
    Deng, Junfeng
    Ji, Qinggang
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023, 255
  • [10] Synthesis, biological evaluation and molecular docking studies of novel quinuclidinone derivatives as potential antimicrobial and anticonvulsant agents
    Laczkowski, Krzysztof Z.
    Landowska, Katarzyna
    Biernasiuk, Anna
    Salat, Kinga
    Furgala, Anna
    Plech, Tomasz
    Malm, Anna
    MEDICINAL CHEMISTRY RESEARCH, 2017, 26 (09) : 2088 - 2104