Author(s):
Ashish Dixit, Pawan Tiwari, Mukesh K. Bhardwaj, Anurag Mishra, Ashwini Mishra
Email(s):
ashdixit05061979@gmail.com
DOI:
10.52711/0974-360X.2026.00587
Address:
Ashish Dixit1*, Pawan Tiwari2, Mukesh K. Bhardwaj3, Anurag Mishra1, Ashwini Mishra1
1Department of Pharmaceutical Chemistry, Spectrum Hi College of Pharmacy, Sultanpur - 228151, Uttar Pradesh, India.
2Department of Pharmaceutical Chemistry, Shambhunath Institute of Pharmacy, Prayagraj - 211015, Uttar Pradesh, India.
3Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Future Institute of Medical Sciences, Future University, Bareilly - 243503, Uttar Pradesh, India.
4Department of Pharmaceutics, Spectrum Hi College of Pharmacy, Sultanpur - 228151, Uttar Pradesh, India.
5Department of Pharmaceutics, Spectrum Hi College of Pharmacy, Sultanpur - 228151, Uttar Pradesh, India.
*Corresponding Author
Published In:
Volume - 19,
Issue - 9,
Year - 2026
ABSTRACT:
Compounds containing pyrazole have shown promise as antioxidants and anti-inflammatory agents because they may be able to block p38a MAP kinase, a crucial therapeutic target in inflammation. The current study sought to synthesize a variety of pyrazole compounds using different synthetic procedures, characterize the synthesized diverse library of pyrazole compounds using spectroscopic techniques such as IR, NMR, and mass spectroscopy, and assess a number of novel pyrazole compounds for their anti-inflammatory activity in vitro using the albumin denaturation inhibition method and their anti-oxidant effect using the DPPH colorimetric technique at a concentration of 1mM to gauge their capacity to scavenge free radicals. The anti-inflammatory properties of the active compounds were confirmed by cell-based assays that showed dose-dependent inhibition of inflammatory markers. When compared to current anti-inflammatory drugs, the most promising compounds showed good cytotoxicity and selectivity profiles. These results demonstrate the potential of pyrazole-based anti-inflammatory and antioxidant moieties as innovative anti-inflammatory drugs. To assess their effectiveness and safety in pertinent disease models, more lead optimization and in vivo research are necessary. This work highlights the significance of pyrazole scaffolds in medicinal chemistry and advances the field of anti-inflammatory drug discovery.
Cite this article:
Ashish Dixit, Pawan Tiwari, Mukesh K. Bhardwaj, Anurag Mishra, Ashwini Mishra. Synthesis of some Novel Pyrazole-derivatives and Evaluation of their Biological Activity as Putative Anti-inflammatory and Antioxidant agent. Research Journal Pharmacy and Technology. 2026;19(9):4201-8. doi: 10.52711/0974-360X.2026.00587
Cite(Electronic):
Ashish Dixit, Pawan Tiwari, Mukesh K. Bhardwaj, Anurag Mishra, Ashwini Mishra. Synthesis of some Novel Pyrazole-derivatives and Evaluation of their Biological Activity as Putative Anti-inflammatory and Antioxidant agent. Research Journal Pharmacy and Technology. 2026;19(9):4201-8. doi: 10.52711/0974-360X.2026.00587 Available on: https://rjptonline.org/AbstractView.aspx?PID=2026-19-9-33
REFERENCES:
1. Nathan Carl. Points of control in inflammation. NATURE. 2002; Vol 420: 846-852. doi: 10.1038/nature01320.
2. Medzhitov Ruslan. Origin and physiological roles of inflammation. NATURE. 2008; Vol 454. 428-435. doi:10.1038/nature0720.
3. Kolls JK, Lindén A. Interleukin-17 family members and inflammation. Immunity. 2004; 21(4): 467–476. doi: 10.1016/j.immuni.2004.08.018.
4. Guangchen Li. Yifu Cheng. Chi Han. Chun Song. Niu Huang and Yunfei Du. Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies. RSC Medicinal Chemistry. 2022: 13, 1300–1321. doi:10.1039/D2MD00206J.
5. Mohammed I. El-Gamal. Seyed-Omar Zaraei. Moustafa M. Madkour and Hanan S. Anbar. Evaluation of Substituted Pyrazole-Based Kinase Inhibitors in One Decade (2011–2020): Current Status and Future Prospects. Molecules. 2022; 27(1): 330; doi: 10.3390/molecules27010330.
6. W. T. Ashton. S. M. Hutchins. W. J. Greenlee. G. A. Doss. R. S. Chang. V. J. Lotti. K. A. Faust, T. B. Chen, G. J. Zingaro and S. D. Kivlighn, J. Med. Chem.,1993; 36: 3595–3605. doi: 10.1021/jm2001585.
7. J. L. Neisewander. R. A. Fuchs. L. E. O'Dell and T. V. Khroyan. Synapse. 1998; 30: 194–204. doi: 10.1002/(sici)1098-2396(199810)30:2J. Hyttel. Eur. J. Pharmacol. 1983; 91: 153–154. doi: 10.1016/0014-2999(83)90054-0.
8. Bouabdallah L.A. M’Barek. A. Zyad. A. Ramdani. I. Zidane. A. Melhaoui. Anticancer effect of three pyrazole derivatives. Natural Product Research. 2006; 20: 1024–1030. doi: 10.1080/14786410600921441.
9. G.M. Nitulescu. C. Draghici. A.V. Missir. Synthesis of new pyrazole derivatives and their anticancer evaluation. European Journal of Medicinal Chemistry. 2010: 45: 4914–4919. doi: 10.1016/j.ejmech.2025.118061.
10. H. Kumar. D. Saini. S. Jain. N. Jain. Pyrazole scaffold: a remarkable tool in the development of anticancer agents. The European Journal of Medicinal Chemistry. 2013; 70: 248–258. doi: 10.1016/j.ejmech.2013.10.004.
11. K. Ando. K. Kawamura. Sulfamoyl hetero aryl Pyrazole Compounds as Anti- Inflammatory/Analgesic Agents. Google Patents. 2003,
12. M. Amir. S. Kumar. Synthesis and anti-inflammatory, Analgesic, ulcerogenic and lipid peroxidation activities of 3, 5-dimethyl pyrazoles, 3-methyl pyrazol-5-ones and 3,5-disubstituted pyrazolines. Indian Journal of Chemistry. 2005; 44B- 2532-2537. doi: 10.1002/chin.200615110.
13. A.A. Farghaly. A.A. Bekhit. J. Young Park. Design and synthesis of some oxadiazolyl, thiadiazolyl, thiazolidinyl, and thiazolyl derivatives of 1H pyrazole as anti-inflammatory antimicrobial agents. Archiv der Pharmazie. 2000;333: 53–57. doi: 10.1002/(SICI)1521-4184(200002)333
14. R.B. Bakr. A.A. Azouz. K.R. Abdellatif. Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of new 1-phenylpyrazolo [3, 4-d]pyrimidine derivatives. Journal of Enzyme Inhibition and Medicinal Chemistry. 2016; 31:6–12. doi: 10.1080/14756366.2016.1186018.
15. K. Abdellatif. E. Abdelall. R. Bakr. Nitric oxide-NASIDS donor prodrugs as hybrid safe anti-inflammatory agents. Current Topics in Medicinal Chemistry. 2017; 17: 941– 955. doi: 10.2174/1568026616666160927153435.
16. Khaled R. A. Abdellatif. Mohamed A. Abdelgawad. Heba A. H. Elshemy. Shahinda S. R. Alsayed. Gehan Kamel. Synthesis and anti-inflammatory evaluation of new 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives possessing an aminosulphonyl pharmacophore. Archives of Pharmacal Research. 2015; 38:1932–1942. doi: 10.1007/s12272-015-0606-7.
17. Rathish I.G. K. Javed S. Ahmad. S. Bano. M.S. Alam. K.K. Pillai. S. Singh. and V. Bagchi. Synthesis and anti-inflammatory activity of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamide. Bioorganic and Medicinal Chemistry Letters. 2009; 19: 255–258. doi: 10.1016/j.bmcl.2008.10.105.
18. Bano S. K. Javed. S. Ahmad. I.G. Rathish. S. Singh. and M.S. Alam. Synthesis and biological evaluation of some new 2-pyrazolines bearing benzene sulfonamide moiety as potential anti-inflammatory and anti-cancer agents. European Journal of Medicinal Chemistry. 2011; 46: 5763–5768. doi: 10.1016/j.ejmech.2011.08.015.
19. Bashir R. S. Ovais. S. Yaseen H. Hamid M.S. Alam M. Samim. S Singh. and K. Javed. Synthesis of some new 1,3,5- trisubstituted pyrazolines bearing benzene sulfonamide as anticancer and anti-inflammatory agents. Bioorganic and Medicinal Chemistry Letters. 2011; 21: 4301–4305. doi: 10.1016/j.bmcl.2011.05.061.
20. Ovais S. R. Bashir. S. Yaseen. P. Rathore. M. Samim. and K. Javed. Synthesis and pharmacological evaluation of some novel 2-pyrazolines bearing benzene sulfonamide as anti-inflammatory and blood glucose lowering agents. Medicinal Chemistry Research. 2012; 22: 1378–1385. doi: 10.1007/S00044-012-0130-Y.
21. Ovais S. S. Yaseen. R. Bashir. P. Rathore. M. Samim. S. Singh. V. Nair. and K. Javed.Synthesis and anti-inflammatory activity of celecoxib like compounds. Journal of Enzyme Inhibition and Medicinal Chemistry. 2013; 28: 1105–1112. doi: 10.3109/14756366.2012.710847.
22. Johnson, M. B. Younglove. L. Lee R. LeBlanc. H.H. Jr. P. Hills. H.Mackay. T. Brown. S.L. Mooberry. and M. Lee. Design, synthesis, and biological testing of pyrazoline derivatives of combretastatin-A4. Bioorganic and medicinal chemistry letters. 2007; 17: 5897–901. doi: 10.1016/j.bmcl.2007.07.105.
23. Rostom, S.A.F. 2006. Synthesis and in vitro antitumor evaluation of some indeno[1,2-c]pyrazol(in)es substituted with sulfonamide, sulfonylurea(-thiourea) pharmacophores, and some derived thiazole ring systems. Bioorganic and Medicinal Chemistry. 14: 6475–6485. doi: 10.1016/j.bmc.2006.06.020.
24. Sahu, S.K. M. Banerjee. A. Samantray. C. Behera. and M.A. Azam. 2008. Synthesis, analgesic, anti-inflammatory and antimicrobial activities of some novel pyrazoline derivatives. Tropical Journal of Pharmaceutical Research. 2008; 7: 961–968. doi: 10.4314/tjpr.v7i2.14664.
25. Chandra T. N. Garg S. Lata K.K. Saxena and A. Kumar. Synthesis of substituted acridinyl pyrazoline derivatives and their evaluation for anti-inflammatory activity. European Journal of Medicinal Chemistry. 2010; 45: 1772–1776. doi: 10.1016/j.ejmech.2010.01.009.
26. Ahn J.H. H.M. Kim. S.H. Jung. S.K. Kang. K.R. Kim. S.D. Rhee.S.D. Yang. H.G. Cheon. and S.S. Kim. Synthesis and DPIV inhibition of cyano-pyrazoline derivatives as potent antidiabetic agents. Bioorganic and Medicinal Chemistry Letters. 2005; 14: 4461–4465. doi: 10.1016/j.bmcl.2004.06.046.
27. Lange J.H.M. H.H.V. Stuivenberg W. Veerman H.C. Wals. B.Stork., H.K.A.C. Coolen. A.C. McCreary. T.J.P. Adolfs. and C.G.Kruse. Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity. Bioorganic and Medicinal Chemistry Letters.2005.15: 4794–4798. doi: 10.1016/j.bmcl.2005.07.054.
28. Xue-Ru Liu. Hua Wu. Ze-Yu He. Zhi-Qing Ma. Jun-Tao Feng. and Xing Zhang. Design, Synthesis and Fungicidal Activities of Some Novel Pyrazole Derivatives. Molecules. 2014; 19-14036-14051; doi:10.3390/molecules190914036.
29. Bettencourt Ana P. Castro Marián. Silva João P. Fernandes Francisco. Coutinho Olga P. Sousa Maria J. Proença Maria F. and Areias Filipe M. Phenolic Imidazole Derivatives with Dual Antioxidant/Antifungal Activity: Synthesis and Structure-Activity Relationship. Medicinal Chemistry.2019; 15(4)-341-351. doi: 10.2174/1573406414666181005143431.
30. Desai Nisheeth C. Patel Bonny Y. Dave Bharti P. Synthesis and antimicrobial activity of novel quinoline derivatives bearing pyrazoline and pyridine analogues. Medicinal Chemistry Research. 2017: 26- 109–119. doi: 10.1007/s00044-016-1732-6.
31. Kumar Parvin. Duhan Meenakshi. Kadyan Kulbir. Bhardwaj Jitender Kumar. Saraf Priyanka. Mittal Meenu. Multicomponent Synthesis of Some Molecular Hybrid Containing Thiazole Pyrazole as Apoptosis Inducer. Drug Research (Stuttg). 2018; 68(02): 72-79. doi: 10.1055/s-0043-116947.
32. Qingyong Li. Jian Chen. Shuyue Luo. Jialin Xu. Qiaoxian Huang. Tianyu Liu. Synthesis and assessment of the antioxidant and antitumor properties of asymmetric curcumin analogues. European Journal of Medicinal Chemistry. 2015; 93-461-469. doi:10.1016/j.ejmech.2015.02.005.
33. Yuan Wang. Mingwei Wu. Chunzhi Ai and Yonghua Wang. Insight into the Structural Determinants of Imidazole Scaffold-Based Derivatives as TNF-α Release Inhibitors by in Silico Explorations. International Journal of Molecular Science. 2015: 16. 20118-20138. doi:10.3390/ijms160920118.
34. Yang C-Y. Hung Y-L. Tang K-W. Wang. S.C. Tseng. C.H. Tzeng. C. C. Liu. P. L. Li C.Y. Chen. Y.L. Discovery of 2-Substituted 3-Arylquinoline Derivatives as Potential Anti-Inflammatory Agents through Inhibition of LPS-Induced Inflammatory Responses in Macrophages. Molecules. 2019; 24: 1162. doi: 10.3390/molecules24061162.
35. Kim K. Kim J.H. Choi H. Lee. B. Lee J. Ok. K.M. Lee, T.H. Kim. H. Synthesis and Anti-Inflammatory Activity of N (2)-Arylindazol-3(2H)-One Derivatives: Copper-Promoted Direct N-Arylation via Chan–Evans–Lam Coupling. Molecules. 2023; 28: 6706. doi: 10.3390/molecules28186706.