ABSTRACT:
A series of four- membered rings has been synthesized from Dapsone drug. In the first step examination Dapsone has been taken as initial material and treated with 4-aminoacetophenone to prepare new Azo compound. then Azo compound reacts with various aromatic amines in absolute ethanol to prepare Schiff bases derivatives. In the second step these derivatives react with Chloroacetylchloride in the presence of tri ethyl amine(Et3N) to prepare new four- membered heterocyclic compounds . All these derivatives were tested against different bacteria(Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, Bacillus anthracis). The high efficacy results of these derivatives proved significantly greater than the efficacy of the same Dapsone drug.These compounds were identified and confirmed by FT- IR, 1HNMRand 13C-NMR.
Cite this article:
Nadia Sadiq Majeed , Fatima Naeem Abdul-Hussein. Preparation, Identification and Evaluation of Biological Activity of some new β-Lactam compounds derived from Schiff bases. Research Journal of Pharmacy and Technology 2023; 16(2):593-6. doi: 10.52711/0974-360X.2023.00101
Cite(Electronic):
Nadia Sadiq Majeed , Fatima Naeem Abdul-Hussein. Preparation, Identification and Evaluation of Biological Activity of some new β-Lactam compounds derived from Schiff bases. Research Journal of Pharmacy and Technology 2023; 16(2):593-6. doi: 10.52711/0974-360X.2023.00101 Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2023-16-2-20
REFERENCES:
1. Hemalatha K. Selvin J.Girija K. Synthesis, In silico Molecular Docking Study and Anti-bacterial Evaluation of some Novel 4-Anilino Quinazolines. Asian J. Pharm. Res. 2018; 8(3): 125-132.DOI: 10.5958/2231-5691.2018.00022.9.
2. Hemalatha K. Raj DN. Begam MF. Sharanya VK. Girija K. Synthesis, Characterization, Docking study and Anti-Bacterial Evaluation of Benzimidazole Derivatives as Biotin Carboxylase Inhibitors. Asian J. Pharm. Tech. 2017; 7(2): 109-114.DOI : 10.5958/2231-5713.2017.00019.8.
3. DaSilva CM. DaSilva DL. Modolo LV. Alves RB. DeResende MA. Martins CVB.DeFátima A. Schiff bases: A short review of their antimicrobial activities. J. Adv. Res.2011; 2: 1–8. DOI: 10.1016/j.jare.2010.05.004
4. Qin W. Long S. Panunzio M. Biondi S. Schiff Bases: A short survey on an evergreen chemistry tool. Molecules. 2013; 18: 12264–12289.DOI: 10.3390/molecules181012264
5. Saillourglensson FG. Chene LR. Hafner SR.Salamon R.Effect of Dapsone on survival in HIV infected patient: ameta-analysis of finished trails. Rev. Epidemiol santepublique. 2000; 48: 17-30.
6. Vander FS. Koten GV. Syntheses of 3- Amino-2-azetidinones: A Literature Survey, Tetrahidron . 1991; 41(36): 7503-7524. DOI: 10.1016/S0040-4020(01)88276-4.
7. Gilchrist, T. Heterocyclic Chemistry. Harlow: Longman Scientific 1987.
8. Ehmann DE. Avibactam is a covalent, reversible, non-β-lactam β-lactamase inhibitor. PNAS. 2012; 109 (29): 11663–11668. DOI: 10.1073/pnas.1205073109.
9. Tidwell T.T. Hugo (Ugo) Schiff, Schiff Bases, and a Century of â-Lactam Synthesis. Angewandte Chemie International Edition, 2008; 47 (6): 1016–1020.DOI: 10.1002/anie.200702965.
10. Staudinger H. Zur Kenntniss der Ketene. Diphenylketen. Justus Liebigs Ann. Chem. 1907;356 (1-2): 51–123. https://doi.org/10.1002/jlac.19073560106.
11. Nangia A. Biradha K. Desiraju GR. Correlation of biological activity in â-lactam antibiotics with Woodward and Cohen structural parameters: A Cambridge database study. J Chem Soc, Perkin Trans.1996; 2(5), 943–53. https://doi.org/10.1039/P29960000943.
12. Salman HH. Abood HS. Ramadhan UH.Synthesis of Some New Azo Compounds of Salicylic Acid Derivatives and Determine Their In Vitro Anti-Inflammatory Activity. Oriental Journal of Chemistry, 2019;35(2): 870-878.DOI: 10.13005/ojc/350251.
13. Muzammil K. Trivedi P. Khetani DB. Synthesis and Characterization of Schiff base m-nitro aniline and their complexes. Res. J. Chem. Sci. 2015; 5(5):52-55.
14. MajeedNS. Mohsen HF. AldujailiRA. Synthesis, characterization and biological activity of some new heterocyclic compounds derived from 4- aminoacetophenone.Biochem. Cell. Arch.2018; 18 (S1): 1107-1116.
15. Mahmood AI. Mahdi HMF.Al-Smaism RF. Comparative studies on Conventional -Microwave assisted synthesis of 2-azetidinone derivatives. IOSR Journal of Pharmacy and Biological Sciences (IOSR-JPBS). 2017; 12 (4):,56-64.DOI: 10.1007/s11094-016-1392-3.
16. Muzammil K. Trivedi P. Khetani DB.Synthesis and Characterization of Schiff base m-nitro aniline and their complexes. Res. J. Chem. Sci. 2015; 5(5), 52-55.
17. Zeki NM., M.Sc.Thesis, University of Mosul, Mosul, Iraq, 2004.
18. Jafar NN, Majeed NS. Microwave assisted synthesis of amide derivatives of the drug ciprofloxacin and screening the biological properties.International Journal of ChemTech Research. 2016; 9(7): 387-395. DOI: 10.17350/HJSE19030000204.
19. Jafar NN, Majeed NS. Microwave-assisted synthesis and biological activity of ester, carbothioate and carbohydrazide derivative compounds of the drug Ciprofloxacin. Journal of Chemical and Pharmaceutical Sciences.2017; 10(1):515-521
20. Mehta PD. Sengar NPS. Subrahmanyam EVS. Satyanarayana D. Synthesis and biological activity studies of some thiazolidinones and azetidinones. Indian Journal of Pharmaceutical Sciences.2006; 68 (1):103-106.DOI: 10.4103/0250-474X.22978.
21. Al-Majidi SMH. Isatin LH. Synthesis, Identification and evaluation of antibacterial activity of some new substituted N-benzyl-5-Bromo Isatin. Journal of Zankoi Sulaimani, 2015; 17(1): 49-59.D.OI: https://doi.org/10.17656/18124100
22. Parmar K. Modi V. Prajapati, S. Patel R. Novel Mannich Products Qunoline Phenyl Azetidin-2-One Synthetic Development and Evalution of Antibacterial Nature. Asian Journal of Biochemical and Pharmaceutical Research.2011; 2 (1):2231-2560.DOI: 10.24214/AJBPR/7/2/3552.
23. Yaqoob RH. Fahad TA. Characterization and antimicrobial activity of new azo complexes containing,paracetamol moiety . World Journal of pharmaceutical Research. 2015; 5(1):35-43.DOI:10.20959.