Synthesis and Biological Evaluation of Some New Benzimidazole Derivatives Bearing Dithiocarbamate Moiety as Potential Cholinesterase Inhibitors

被引:0
|
作者
Abu Mohsen, Usama [1 ]
机构
[1] Al Azhar Univ, Fac Pharm, Dept Pharmaceut Chem, Gaza, Palestine
来源
CUKUROVA MEDICAL JOURNAL | 2014年 / 39卷 / 04期
关键词
Benzimidazole; Dithiocarbamate; Anticholinesterase Activity;
D O I
暂无
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
Purpose: The synthesis of eight new benzimidazole derivatives bearing dithiocarbamate moiety and subsequently their anticholinesterase activity evaluations were aimed in this present study. Material and Methods: 2-Bromoacetylbenzimidazole react with dithiocarbamate salt derivatives and the resulted compounds were elucidated by 1H NMR, mass spectral data, and elemental analyses. Each derivative was evaluated for its ability to inhibit acetylcholinesterase (AChE) in vitro by using a modification of Ellman's spectrophotometric method. Results: The new compound1-methyl-2{2'[(N, Ndimethylaminothiocarbamoylthio)-acetyl]} benzimidazole (2b) can be identified as promising anticholinesterase agent in vitro due to its moderate inhibition effect, which is about 37%, when compared with standard substance Donepezil under the same experimental conditions. Conclusion: In comparing with the reference standard, among the synthesized eight new compounds the only compound namely 1-methyl-2{2'[( N, Ndimethylaminothiocarbamoyl-thio)-acetyl]} benzimidazole (2b) has a promising anticholinesterase activity.
引用
收藏
页码:729 / 735
页数:7
相关论文
共 50 条
  • [1] Synthesis and Biological Evaluation of Some Pyrazoline Derivatives Bearing a Dithiocarbamate Moiety as New Cholinesterase Inhibitors
    Altintop, Mehlika D.
    Ozdemir, Ahmet
    Kaplancikli, Zafer A.
    Turan-Zitouni, Guelhan
    Temel, Halide E.
    Ciftci, Guelsen A.
    ARCHIV DER PHARMAZIE, 2013, 346 (03) : 189 - 199
  • [2] Synthesis and biological evaluation of some thiazole derivatives as new cholinesterase inhibitors
    Turan-Zitouni, Gulhan
    Ozdemir, Ahmet
    Kaplancikli, Zafer Asim
    Altintop, Mehlika Dilek
    Temel, Halide Edip
    Ciftci, Gulsen Akalin
    JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2013, 28 (03) : 509 - 514
  • [3] Synthesis and Evaluation of Some Novel Benzimidazole Derivatives Bearing Thiazolidinone Moiety as Potential Antimicrobial Activity
    Kumar, P. Sudhir
    Patro, S. K.
    ASIAN JOURNAL OF CHEMISTRY, 2013, 25 (18) : 10449 - 10453
  • [4] Synthesis and antibacterial evaluation of new sulfanyltetrazole derivatives bearing piperidine dithiocarbamate moiety
    Baghershiroudi, Mahrokh
    Safa, Kazem D.
    Adibkia, Khosro
    Lotfipour, Farzaneh
    SYNTHETIC COMMUNICATIONS, 2018, 48 (03) : 323 - 328
  • [5] Design, Synthesis, and Biological Evaluation of Some Benzothiazolone Derivatives as Cholinesterase Inhibitors
    Alagoz, Mehmet Abdullah
    Akkaya, Didem
    Arslan, Gulnur
    Uludag, Berk
    Ozdemir, Zeynep
    Barut, Burak
    Onkol, Tijen
    Sari, Suat
    CHEMISTRYSELECT, 2022, 7 (46):
  • [6] Synthesis and Biological Evaluation of Some New Amide Moiety Bearing Quinoxaline Derivatives as Antimicrobial Agents
    Abu Mohsen, U.
    Yurttas, L.
    Acar, U.
    Ozkay, Y.
    Kaplancikli, Z. A.
    Gencer, H. Karaca
    Canturk, Z.
    DRUG RESEARCH, 2015, 65 (05) : 266 - 271
  • [7] Synthesis, docking study and biological evaluation of some new thiourea derivatives bearing benzenesulfonamide moiety
    Ghorab, Mostafa M.
    El-Gaby, Mohamed S. A.
    Soliman, Aiten M.
    Alsaid, Mansour S.
    Abdel-Aziz, Marwa M.
    Elaasser, Mahmoud M.
    CHEMISTRY CENTRAL JOURNAL, 2017, 11
  • [8] Synthesis, docking study and biological evaluation of some new thiourea derivatives bearing benzenesulfonamide moiety
    Mostafa M. Ghorab
    Mohamed S. A. El-Gaby
    Aiten M. Soliman
    Mansour S. Alsaid
    Marwa M. Abdel-Aziz
    Mahmoud M. Elaasser
    Chemistry Central Journal, 11
  • [9] Biological evaluation of some tetrazole derivatives as cholinesterase inhibitors
    Abu Mohsen, Usama
    Yurttas, Leyla
    Ozdemir, Ahmet
    Turan-Zitouni, Gulhan
    Kaplancikli, Zafer Asim
    CLINICAL AND EXPERIMENTAL HEALTH SCIENCES, 2014, 4 (01): : 1 - 4
  • [10] Arylaminopropanone Derivatives as Potential Cholinesterase Inhibitors: Synthesis, Docking Study and Biological Evaluation
    Hudcova, Anna
    Kroutil, Ales
    Kubinova, Renata
    Garro, Adriana D.
    Gutierrez, Lucas J.
    Enriz, Daniel
    Oravec, Michal
    Csollei, Jozef
    MOLECULES, 2020, 25 (07):