Deepika. P, D. Uma Maheshwari, M. Kumar, B. S. Venkateswarlu, Vimal. K. R
Deepika. P*1, D. Uma Maheshwari2, M. Kumar3, B. S. Venkateswarlu4, Vimal. K. R5
1Ph.D Research Scholar, Department of Pharmaceutical Chemistry, Vinayaka Missions College of Pharmacy, Salem, Tamil Nadu, India.
1Associate Professor, Jamia Salafiya Pharmacy College, Pulikkal, Malappuram, Kerala – 673637.
2,3,4Professor, Vinayaka Missions College of Pharmacy, Salem, Tamil Nadu, India – 636008.
5Assistant Professor, Devaki Amma Memorial College of Pharmacy, Chelembra, Malappuram – 673634.
Volume - 15,
Issue - 7,
Year - 2022
A series of pyrazoline comprising coumarin moiety was docked against Mycobacterium tuberculosis shikimate kinase which is an essential target for novel anti tubercular drug design. When the designed pyrazoline containing coumarin derivatives were docked with the receptor (1U8A), the docking scores obtained were greater than the natural ligand and the standards of some derivatives. A number of substituted chalcones were synthesized from thiophene-2-carboxaldehyde by condensing with various substituted acetophenones in presence of sodium hydroxide as a base. Pyrazoline derivatives were prepared by the condensation of chalcones with coumarin carbohydrazide in the presence of ethanol as the catalyst. The structures of the final synthesized compounds were confirmed by spectral analysis. Analogue 3a showed profound antitubercular activity against the organism at lower concentration.
Cite this article:
Deepika. P, D. Uma Maheshwari, M. Kumar, B. S. Venkateswarlu, Vimal. K. R. Design, Synthesis and Antitubercular Study of Novel Pyrazoline Moiety as Mycobacterium Tuberculosis shikimate kinase inhibitor. Research Journal of Pharmacy and Technology. 2022; 15(7):2895-7. doi: 10.52711/0974-360X.2022.00483
Deepika. P, D. Uma Maheshwari, M. Kumar, B. S. Venkateswarlu, Vimal. K. R. Design, Synthesis and Antitubercular Study of Novel Pyrazoline Moiety as Mycobacterium Tuberculosis shikimate kinase inhibitor. Research Journal of Pharmacy and Technology. 2022; 15(7):2895-7. doi: 10.52711/0974-360X.2022.00483 Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2022-15-7-5
1. Ying Zhang.Katrin. Post-Martens. Steven Denkin. New drug candidates and therapeutic targets for tuberculosis therapy.DDT.2006; 11(2): 21-23. doi: 10.1016/S1359-6446(05)03626-3
2. Tuberculosis control in South East Asia region. World Health Organization report. 2012: 1-3.
3. Yar MS. Anees Siddiqui. Ashraf Ali Mohamed. Synthesis and antimycobacterial activity of novel heterocycles. J. Serb. Chem. Soc. 2007; 72 (1): 5–11. doi:10.2298/JSC0701005Y
4. Karthikeyan MS.Bantwal Shivarama. Nalilu Suchetha Kumari. Synthesis and antimicrobial studies on novel chloro-fluorine containing hydroxy pyrazolines. E. J. Med. Chem. 2007; 42: 30- 36. doi:10.1016/j.ejmech.2006.07.011
5. Dmytro Havrylyuk. Lesyk R. Borys Zimenkovsky.et al., Synthesis of novel thiazolone-based compounds containing pyrazoline moiety and evaluation of their anticancer activity. E. J. Med. Chem. 2009; 44(4): 1396-404. doi: 10.1016/j.ejmech.2008.09.032
6. K. Ishwar Bhat. Abishek Kumar. Synthesis and biological evaluation of some novel pyrazoline derivatives derived from chalcones. Research Journal of Pharmacy and Technology.2017;10(5);1344-1346.doi: 10.5958/0974-360X.2017.00238.4
7. Negihan Beyhan. Bedia Kocyigit. Salih Gumuru.et al., Synthesis and Anticonvulsant Activity of Some 2-pyrazolines derived from chalcones. Arabian journal of chemistry.2013;doi.org/10.1016/j.arabjc.2013.07.037
8. Bindu Sree Koduru.Akshay R Shinde. Jaya preeti. Pavan Kumar.et al., Synthesis, Characterization, Anti-tubercular, Analgesic and Anti-Inflammatory Activities of New 2- Pyrazoline Derivatives. Asian J. Pharm. Tech.2012; 2(2);47-50.Available on: https://ajptonline.com/AbstractView.aspx?PID=2012-2-2-4
9. Gummudavelly Sandeep. Sri Ranganath. S Bhaskar. et al., Synthesis and Biological Screening of Some Novel Coumarin Derivatives. Asian J. Research Chem. 2009; 2(1); 46-48. Available on:.https://ajrconline.org/AbstractView.aspx?PID=2009-2-1-11
10. S. Ramachandran.Vijey Anandhi. Binoy Varghese Cherian.et al., Assessment of Antitubercular Activity- A Review. Research J. Pharm. and Tech.2019; 12(8):3973-3978. doi: 10.5958/0974-360X.2019.00684.X
11. Jacob Jincy.Dey Thathagata.Ghate Manjunath.et al., Synthesis of Some Novel Coumarino Benzimidazoles Derivatives for Anti-Inflammatory Screening. Asian J. Research Chem.2010; 3(1);116-120
12. Afnan E. Abd-Almonium. Shaimaa Mohammed.et al., Preparation, Characterization and Antioxidant Determination of Coumarin Substituted Heterocyclic Compound. Asian J. Research Chem. 2020; 13(1): 23-27. doi: 10.5958/0974-4150.2020.00006.1
13. Sanjib Das.R.C.Das.S.H.Bhosale.et al., Synthesis and Pharmacological Evaluation of Atypical Antipsychotic Activity of New Coumarinoacetamides. Asian J. Research Chem.2010; 3(1): 166-171. Available on: https://ajrconline.org/AbstractView.aspx?PID=2010-3-1-43
14. Shubhangi S. Soman. Tirth. H. Thaker. Radhika Baloni. et al., Synthesis of Aminoacetylcoumarins and Aminoacetylnaphthocoumarins and their Antibacterial activity study. Asian J. Research Chem. 2011; 4(1): 132-136.
15. K. Ishwar Bhat.Apoorva. A. Abhishek Kumar. et al., Synthesis and Antidiabetic Evaluation of Some New Coumarin Coupled 4-Thiazolidinone Derivatives. Research J. Pharm. and Tech. 2019; 12(11): 5215-5218. doi: 10.5958/0974-360X.2019.00902.8
16. B. C. Revanasiddappa. E. V. S. Subrahmanyam. T. N. Lakshmi. Synthesis and biological evaluation of some novel pyrazolines. Indian Journal of Pharmaceutical Education and Research.2011; 45(2): 164-166. Available on: http://www.ijper.org/article/324
17. Rama Ganesh CK.Bodke.Yadav.D.et al., Synthesis and biological evaluvation of some innovative coumarin derivative containing thiazoline -4- one ring. Indian Journal of Chemistry.2010; 49B: 1151-1154.Available on: http://nopr.niscair.res.in/handle/123456789/10089