Author(s):
Kumaraswamy Gullapelli, Ravichandar Maroju, Ramchander Merugu
Email(s):
kumargullapelli001@gmail.com
DOI:
10.52711/0974-360X.2021.00738 
Address:
Kumaraswamy Gullapelli1*, Ravichandar Maroju1, Ramchander Merugu2
1Dept. of Chemistry, Mahatma Gandhi Institute of Technology, Hyderabad – 500075.
2Dept. of Biochemistry, Mahatma Gandhi University, Nalgonda – 508254.
*Corresponding Author
Published In:
Volume - 14,
Issue - 8,
Year - 2021
ABSTRACT:
The present study is aiming at synthesis of new heterocycles like benzimidazole nucleus containing Pyrazole, isoxazole and thiazoles. The title compounds were synthesized from 4-(1H-benzo[d]imidazol-2-yl) oxazol-2-amine (1). The title compounds were evaluated for their in vitro anti-inflammatory activity and showed excellent to moderate activity and molecular docking studies were supporting anti-inflammatory activity exhibiting high inhibition constant and binding energy. The chemical structures of the synthesised compounds were characterized by IR, 1HNMR, Mass spectroscopic techniques.
Cite this article:
Kumaraswamy Gullapelli, Ravichandar Maroju, Ramchander Merugu. Synthesis, In-vitro and In-silico Anti-inflammatory activity of new Thiazole derivatives. Research Journal of Pharmacy and Technology. 2021; 14(8):4253-0. doi: 10.52711/0974-360X.2021.00738
Cite(Electronic):
Kumaraswamy Gullapelli, Ravichandar Maroju, Ramchander Merugu. Synthesis, In-vitro and In-silico Anti-inflammatory activity of new Thiazole derivatives. Research Journal of Pharmacy and Technology. 2021; 14(8):4253-0. doi: 10.52711/0974-360X.2021.00738 Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2021-14-8-44
REFERENCES:
1. Valery AC and Fokin V, Organic synthesis On Water. Chemical Reviews, 2009; 109(2): 725-748. DOI: 10.1021/cr 800448q
2. Jiang B, Rajale T, Wever W, Jiang S. Multicomponent reactions for the synthesis of heterocycles. Chemistry. An Asian Journal. 2010; 5(11): 2318-2335. DOI: 10.1002/ asia. 201000310.
3. Singh A K, Ekta K , Chauhan H S . Evaluation of Benzimidazole Derivatives by using Aldehydes. Research J. Pharm. and Tech. 2014; 7(6): 677-685.
4. Gullapelli K, Brahmeshwari G, Ravichandar M. A Facile synthesis of 1-Aryl pyrroles by Clauson Kaas reaction using oxone as a catalyst under microwave irradiation. Bull. Chem. Soc. Ethiop. 2019; 33(1): 143-148.
5. Varsha A D , Rohini R P. Synthesis of some Sulphur and Nitrogen containing Heterocyclic Compounds. Asian J. Pharm. Res. 2017; 7(1): 21-24.
6. Gullapelli K, Bhaskar P, Brahmeshwari G, Synthesis and antibacterial activity of substituted -1-(tosyl/methylsulphonyl-1Hindole-2-yl) methyl 1-H-Indoles. Asian J. Research Chem. 2014; 7(5): 509-512.
7. Gullapelli K, Ravichandar M, Bhasker P, Jagadeesh K, Brahmeshwarri G. Synthesis of 1,3,5 triazinane-2-ones and 1,3,5 oxadiazinane -2-ones linked with Benzimidazoles. Asian J. Research Chem. 2017; 10(4): 513-516.
8. Hassan S, Thamson Müller JJ. Multicomponent syntheses based up on copper catalyzed alkyne –azide Cycloaddition, Advanced Synthesis and Catalysis, 2015; 357(4): 617-666, DOI: 10.1002/adsc.201400904.
9. Sherif Rostam AF, EI –Ashmawy IM, Heba. Abd EI Razik A , Mona H. Badr, Hayam Ashour M A. Design and synthesis of some thiazolyl and thiadiazolyl derivatives of antipyrine as potential non-acidic anti-inflammatory, analgesic and antimicrobial agents. Bioorganic and Medicinal Chemistry, 2009; 17(2): 882-895, DOI: 10:1016/ jbmc 2008. 11.035.
10. Mukhtyar. S. Saini, A. Kumar, J. Dwivedi, R. Singh. A Review: Biological significances of heterocyclic compounds Int J Pharm Sci Rev Res, 2013; 4(3): 66-77.
11. Prabha T, Aishwaryah P, Manickavalli E, Chandru R, Arulbharathi G, Anu A, Sivakumar T. A Chalcone Annulated Pyrazoline Conjugates as a Potent Antimycobacterial Agents: Synthesis and in Silico Molecular Modeling Studies. Research J. Pharm. and Tech. 2019; 12(8): 3857-3865.
12. Kalkotwar R S, Saudagar R B. Design and, synthesis and antimicrobial, anti-inflammatory, Antitubercular activities of some 2,4,5 –trisubstituted imidazole derivatives. Asian J Pharm. Res. 2013; 3(4): 159-165.
13. Galal SA, Abdelsamie AS, Rodriguez ML, Kerwin SM, Diwani HI. Synthesis and studying the antitumor activity of novel 5-(2-methyl benzimidazole-5-yl)-1,3,4 –oxadiazole-2 (3H)-thiones, European Journal of Chemistry. 2010; 1(2): 67-72, DOI: 10. 5155/ eurjchem.1.2.67-72.1.
14. Gullapelli K, Brahmeshwari G. Synthesis and antifungal activity of 3-(4-(4(1H-Benzo(d) imidazole -2-yl ) phenyl amino )thiazol-2-yl)2-phenyl thiazolidin -4-one derivatives , Int. J. Chem. Sci. 2014; 12(3): 885-893.
15. I. M. Madawali, K. K. Das, E. N. Gaviraj, N. V. Kalyane, B. Shivakumar, Synthesis and evaluation of 4-(1H-Benzimidazol-2yl)-6-(2-chloroquinolin-3-yl) pyrimidin -2-amine as potent anthelmintic agents. J. Chem. Pharm. Res. 2018; 10: 76–83.
16. Nadeem S, Shamsher Alam M D, Meeta S , Shahar Yar M , Ozair A, Jamshed Ahmad Siddiqui M D. Antidepressant, Analgesic Activity and SAR Studies of Substituted Benzimidazoles. Asian J. Pharm. Res. 2016; 6(3): 170-174.
17. Dixit S, Kumar Sharma P, Kaushik N. Synthesis of Novel Benzimidazole Derivatives: As Potent Analgesic Agent, Medicinal Chemistry Research. 2013; 22(2): 900-904, DOI: 10.1007/s00044-012-0083-1.
18. Hitesh V. S, Rakesh D. A. Synthesis, Characterization and Antimicrobial Activity of Diphenylamino Isoxazoline Derivatives. Asian J. Pharm. Res. 2018; 8(3): 148-150.
19. Ngono Bikob D S, Vodnar D C , Stana A, Tiperciuc B, Nastasa C, Douchet M, Oniga O, Synthesis of 2-phenylamino-thiazole derivatives as antimicrobial agents. Journal of Saudi Chemical Society. 2017; 21(7): 861-868., DOI:10.1016/ j. jscs. 2017. 04.007
20. Hemalatha K, Niranjan Raj D, Fousia Begam M, Sharanya V K , 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.
21. Gupta V , Girendra Kumar G ,Yadav S K . Synthesis, Characterization and Evaluation of substituted Benzimidazole hydrazine Carboxamide derivatives for Anti-inflammatory activity. Int. J. Tech. 2017; 7(2): 90-95.
22. Gullapelli K, Brahmeshwari G, Ravichander M, Uma K. Synthesis, antibacterial and molecular docking studies of new benzimidazole derivatives, Egypt J. Basic and Applied sciences., 2017; 4 (4): 303-309 . DOI:10.1016/j.ejbas.2017.09.002.
23. Sangita Ch, Priyanka Ch, Protapaditya D, Bhattacharya S. Evaluation of Anti-inflammatory Effect of Ashwagandha: A Preliminary Study in vitro. Pharmacognosy Journal. 2012; 4: 47-49.
24. Bikadi Z, Demko L and Hazai E. Functional and structural characterization of a protein based on analysis of its hydrogen bonding network by hydrogen bonding plot. Arch. Biochem. Biophys. 2007; 461: 225-234.
25. Bikadi Z, Hazai E. Application of the PM6 semi-empirical method to modelling proteins enhances docking accuracy of Auto Dock, J. Chem Inf. 2009; 1: 15.
26. K. Gullapelli, K. Dhanaja, M. Ravichander, M. Ramachander. G. Brahmeshwari, Synthesis, antitubercular and molecular docking studies of new biheterocyclic compounds on benzimidazole moiety, Rasayan J. Chem., 2020; 13(1): 585-592. doi.org/10.31788/ RJC. 2020. 1315465.