Volume : 13, Issue : 07, July – 2026
Title:
DESIGN, SYNTHESIS, CHARACTERIZATION AND IN-VITROANTI-INFLAMMATORY EVALUATION OF NOVEL INDOLE DERIVATIVES.
Authors :
Rutuja S. Pattekar, Prachi.P. Kanawade
Abstract :
Since inflammation is a complicated biological reaction linked to a wide range of acute and chronic illnesses, there is an ongoing need to produce safer and more potent anti-inflammatory drugs. A unique heterocyclic scaffold, indole is well known for its vast range of biological actions, including strong anti-inflammatory potential. A number of novel indole derivatives were logically designed and synthesized in the current work using suitable synthetic techniques. Physicochemical and spectroscopic methods, such as melting point determination, Fourier Transform Infrared (FT-IR) spectroscopy, Nuclear Magnetic Resonance (^1H NMR and ^13C NMR) spectroscopy, and Mass Spectrometry (MS), were used to purify and characterize the synthesized compounds and confirm their chemical structures. Diclofenac sodium was used as the reference standard in conventional assays, such as suppression of protein denaturation and membrane stabilization techniques, to assess the synthesized derivatives’ in-vitro anti-inflammatory effectiveness. Several synthetic compounds showed promise anti-inflammatory activity, according to the biological evaluation, and some derivatives showed inhibition that was similar to that of the standard medication. The kind and location of substituents on the indole nucleus had a major impact on the anti-inflammatory efficacy, according to preliminary structure–activity relationship (SAR) research.
These new indole derivatives appear to be attractive lead compounds for the creation of novel anti-inflammatory drugs. To determine their therapeutic potential and improve their pharmacological profile, more in-vivo pharmacological research, toxicity evaluations, and molecular docking studies are necessary.
Keywords: Indole, anti-inflammatory, spectroscopy, therapeutic, Nuclear Magnetic Resonance.
Cite This Article:
Please cite this article in press Rutuja S. Pattekar et al., Design, Synthesis, Characterization And In-Vitroanti-Inflammatory Evaluation Of Novel Indole Derivatives, Indo Am. J. P. Sci, 2026; 13(07).
REFERENCES:
1. de Martel C, Maucort-Boulch D, Plummer M, Franceschi S. World-wide relative contribution of Helicobacter pylori and hepatitis B and C viruses in gastric cancer. Int J Cancer. 2015;136(6):487–490. doi:10.1002/ijc.28999.
2. Kaushik NK, Kaushik N, Attri P, Kumar N, Kim CH, Verma AK, et al. Biomedical importance of indoles. Molecules. 2013;18(6):6620–6662. doi:10.3390/molecules18066620.
3. Kumari A, Singh RK. Medicinal chemistry of indole derivatives: Current to future therapeutic perspectives. Bioorg Chem. 2019;89:103021.
4. Chadha N, Silakari O. Indoles as therapeutics of interest in medicinal chemistry: Bird’s eye view. Eur J Med Chem. 2017;134:159–184.
5. Sharma V, Kumar P, Pathak D. Biological importance of the indole nucleus in recent years: A comprehensive review. J Heterocycl Chem. 2010;47(3):491–502.
6. Kaur M, Singh M, Chadha N, Silakari O. Oxindole: A promising scaffold for the development of anti-inflammatory agents. Eur J Med Chem. 2016;123:858–894.
7. Rane RA, Gutte SD, Sahu NU. Synthesis and biological evaluation of novel indole derivatives as anti-inflammatory agents. Bioorg Med Chem Lett. 2012;22:6429–6432.
8. Kumar S, Bawa S, Gupta H. Biological activities of indole derivatives: A review. Mini Rev Med Chem. 2009;9(14):1648–1654.
9. Bandgar BP, Gawande SS, Bodade RG, Totre JV, Khobragade CN. Synthesis and biological evaluation of simple methoxylated chalcones as anti-inflammatory agents. Bioorg Med Chem. 2010;18(3):1364–1370.
10. Monks A, Scudiero D, Skehan P, et al. Feasibility of a high-flux anticancer drug screen using a diverse panel of cultured human tumor cell lines. J Natl Cancer Inst. 1991;83(11):757–766. doi:10.1093/jnci/83.11.757.
11. Kaushik NK, Kaushik N, Attri P, Kumar N, Kim CH, Verma AK, et al. Biomedical importance of indoles. Molecules. 2013;18(6):6620–6662. doi:10.3390/molecules18066620.
12. Chadha N, Silakari O. Indoles as therapeutics of interest in medicinal chemistry: Bird’s eye view. Eur J Med Chem. 2017;134:159–184.
13. Kumari A, Singh RK. Medicinal chemistry of indole derivatives: Current to future therapeutic perspectives. Bioorg Chem. 2019;89:103021.
14. Vane JR, Botting RM. Mechanism of action of anti-inflammatory drugs. Int J Tissue React. 1998;20:3–15.
15. Ricciotti E, FitzGerald GA. Prostaglandins and inflammation. Arterioscler Thromb Vasc Biol. 2011;31(5):986–1000. doi:10.1161/ATVBAHA.110.207449.
16. Lionta E, Spyrou G, Vassilatis DK, Cournia Z. Structure-based virtual screening for drug discovery. Curr Top Med Chem. 2014;14(16):1923–1938. doi:10.2174/1568026614666140929124445.
17. Langer T, Hoffmann RD. Virtual Screening: An Effective Tool for Lead Structure Discovery? Weinheim: Wiley-VCH; 2006.
18. Meanwell NA. Improving drug candidates by design: A focus on bioisosteres. J Med Chem. 2011;54(8):2529–2591. doi:10.1021/jm1013693.
19. Morris GM, Huey R, Lindstrom W, et al. AutoDock4 and AutoDockTools4: Automated docking with selective receptor flexibility. J Comput Chem. 2009;30(16):2785–2791. doi:10.1002/jcc.21256.
20. Daina A, Michielin O, Zoete V. SwissADME: A free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules. Sci Rep. 2017;7:42717. doi:10.1038/srep42717.
21. Pires DEV, Blundell TL, Ascher DB. pkCSM: Predicting small-molecule pharmacokinetic and toxicity properties using graph-based signatures. J Med Chem. 2015;58(9):4066–4072. doi:10.1021/acs.jmedchem.5b00104.
22. Robinson B. The Fischer indole synthesis. Chem Rev. 1963;63(4):373–401. doi:10.1021/cr60224a002.
23. Bartoli G, Palmieri G, Bosco M, Dalpozzo R. Bartoli indole synthesis. Tetrahedron. 1990;46:4221–4256.
24. Cacchi S, Fabrizi G. Synthesis and functionalization of indoles through palladium catalysis. Chem Rev. 2005;105(8):2873–2920. doi:10.1021/cr040639b.
25. Furniss BS, Hannaford AJ, Smith PWG, Tatchell AR. Vogel’s Textbook of Practical Organic Chemistry. 5th ed. Harlow: Pearson Education.
26. Mizushima Y, Kobayashi M. Interaction of anti-inflammatory drugs with serum proteins. J Pharm Pharmacol. 1968;20(3):169–173.
27. Shinde UA, Phadke AS, Nair AM, et al. Membrane stabilization activity: A possible mechanism of anti-inflammatory action. Fitoterapia. 1999;70(3):251–257.
28. Oyedepo OO, Femurewa AJ. Anti-protease activity as a mechanism of anti-inflammatory action. Int J Pharmacogn. 1995;33:65–69.
29. Axelrod B, Cheesbrough TM, Laakso S. Lipoxygenase from soybeans. Methods Enzymol. 1981;71:441–451.
30. Warner TD, Mitchell JA. Cyclooxygenases: New forms, new inhibitors, and lessons from the clinic. FASEB J. 2004;18(7):790–804. doi:10.1096/fj.03-0645rev.




