Volume : 13, Issue : 09, September – 2026
Title:
COUMARIN DERIVATIVES AS PROMISING THERAPEUTIC AGENTS AN UPDATED REVIEW
Authors :
Mallikarjun H, Kartik Havale, Sandhya D. Chinnamulagund*, Tabasum Killedar, V. H. Kulkarni, Shrinivas D. Joshi
Abstract :
Coumarin (2H-chromen-2-one) is a naturally occurring benzopyrone compound that has attracted considerable attention because of its wide range of biological activities and its importance in medicinal chemistry. Owing to its versatile chemical structure, coumarin serves as a valuable scaffold for the development of numerous therapeutically active compounds. This review provides an overview of the physicochemical and spectroscopic properties of coumarin, along with the major synthetic methods, including the Perkin, Pechmann, Kostanecki–Robinson, and Claisen rearrangement reactions. The characteristic IR and 1H NMR spectral features used for the identification and structural confirmation of coumarin are also discussed. In addition, recent advances in the synthesis and biological evaluation of coumarin derivatives are summarized, highlighting their antimicrobial, antibacterial, antifungal, anti-tubercular, antioxidant, and anticancer activities. The review also discusses how structural modifications of the coumarin nucleus influence biological activity and improve therapeutic potential. Furthermore, selected commercially available coumarin derivatives and their pharmaceutical significance are briefly described. Overall, this review highlights the growing importance of coumarin as a versatile heterocyclic scaffold and its continued potential in the discovery and development of new bioactive molecules.
Keywords: Coumarin, Heterocyclic compounds, Medicinal chemistry, Drug discovery, Biological activity.
Cite This Article:
Please cite this article in press Sandhya D C et al., Coumarin Derivatives As Promising Therapeutic Agents An Updated Review.,. Indo Am. J. P. Sci, 2026; 13(10).
REFERENCES:
[1] Murray RDH., Méndez J., Brown SA. The natura, coumarins: Occurrence, Chemistry and Biochemistry. 1983; 702.
[2] Venugopala KN, Rashmi V, Odhav B. Review on Natural Coumarin Lead Compounds for Their Pharmacological Activity. Biomed Res Int 2013; 2013: 963248.
[3] Borges F, Roleira F, Milhazes N, et al. Simple Coumarins and Analogues in Medicinal Chemistry: Occurrence, Synthesis and Biological Activity. Curr Med Chem 2005; 12: 887–916.
[4] Emami S, Dadashpour S. Current developments of coumarin-based anti-cancer agents in medicinal chemistry. Eur J Med Chem 2015; 102: 611–630.
[5] Kumar A, Baccoli R, Fais A, et al. Substitution Effects on the Optoelectronic Properties of Coumarin Derivatives. Appl Sci; 10. Epub ahead of print 1 January 2019. DOI: 10.3390/APP10010144.
[6] dos Santos RR, Turra B, Simon K, et al. Evaluation of genotoxicity and coumarin production in conventional and organic cultivation systems of Mikania glomerata Spreng. J Environ Sci Heal Part B 2019; 54: 866–874.
[7] IJSRST, Pankaj S. Borkar, Sangharsh S. Chandekar, et al. International Journal of Scientific Research in Science and Technology. Int J Sci Res Sci Technol 2008; 1: 1.
[8] Lei L, Yang D, Liu Z, et al. Mono‐nitration of Coumarins by Nitric Oxide. Synth Commun 2004; 34: 985–992.
[9] Perkin WH. IV.—On some new derivatives of coumarin. J Chem Soc 1871; 24: 37–55.
[10] Clayton A. CXXVIII.—The action of alkalis on certain derivatives of coumarin. J Chem Soc, Trans 1910; 97: 1388–1408.
[11] Kumar, P. Sudhir; Ghosh, G.; Rout, S. K.; Paul D. Synthesis and antimicrobial evaluation of some novel 4-hydroxy coumarin derivatives bearing azo moiety. Rasayan J Chem 2013; 6: 147–152.
[12] Singh I, Kaur H, Kumar S, et al. Synthesis of New Coumarin Derivatives as Antibacterial Agents. Int J ChemTech Res CODEN( USA; 2: 1745–1752.
[13] Regal MKA, Shaban SS, El-Metwally SA. Synthesis and Antimicrobial Activity of Some New Coumarin and Dicoumarol Derivatives. Russ J Bioorganic Chem 2020; 46: 438–447.
[14] Kudale SD, Deodhar MN. Synthesis and evaluation of some coumarin containing potential antimicrobial agents. E-Journal Chem 2012; 9: 2493–2500.
[15] Dekić BR, Radulović NS, Dekić VS, et al. Synthesis and antimicrobial activity of new 4-heteroarylamino coumarin derivatives containing nitrogen and sulfur as heteroatoms. Molecules 2010; 15: 2246–2256.
[16] Naik CG, Malik GM, Parekh HM. Novel coumarin derivatives: Synthesis, characterization and antimicrobial activity. South African J Chem 2019; 72: 248–252.
[17] Al-Haiza MA, Mostafa MS, El-Kady MY. Synthesis and biological evaluation of some new coumarin derivatives. Molecules 2003; 8: 275–286.
[18] Kulkarni A, Patil SA, Badami PS. Synthesis, characterization, DNA cleavage and in vitro antimicrobial studies of La(III), Th(IV) and VO(IV) complexes with Schiff bases of coumarin derivatives. Eur J Med Chem 2009; 44: 2904–2912.
[19] Rehman S, Ikram M, Baker RJ, et al. Synthesis, characterization, in vitro antimicrobial, and U2OS tumoricidal activities of different coumarin derivatives. Chem Cent J 2013; 7: 68.
[20] Arshad A, Osman H, Bagley MC, et al. Synthesis and antimicrobial properties of some new thiazolyl coumarin derivatives. Eur J Med Chem 2011; 46: 3788–3794.
[21] Sahoo SS, Shukla S, Nandy S, et al. Synthesis of novel coumarin derivatives and its biological evaluations. Eur J Exp Biol 2012; 2: 899–908.
[22] Abduljabbar TT, Hadi MK. Synthesis, Characterization and Antibacterial Evaluation of Some Coumarin Derivatives. Iraqi J Pharm Sci 2021; 30: 249–257.
[23] Betti N, Shia JS, Kadhum AAH, et al. Harnessing coumarin chemistry: Antibacterial, antifungal, and antioxidant profiling of novel coumarin derivatives. J Med Pharm Chem Res 2024; 6: 1530–1546.
[24] Wili P. Coumarin – Dithiocarbamate Derivatives as Biological Agents. 2025; 1–15.
[25] Reddy DS, Kongot M, Netalkar SP, et al. Synthesis and evaluation of novel coumarin-oxime ethers as potential anti-tubercular agents: Their DNA cleavage ability and BSA interaction study. Eur J Med Chem 2018; 150: 864–875.
[26] Phutdhawong W, Chuenchid A, Taechowisan T, et al. Synthesis and Biological Activity Evaluation of Coumarin-3-. Molecules 2021; 26: 1–12.
[27] Al-Hazmy SM, Zouaghi MO, Al-Johani JN, et al. Chemosensing Properties of Coumarin Derivatives: Promising Agents with Diverse Pharmacological Properties, Docking and DFT Investigation. Molecules 2022; 27: 1–31.
[28] Quadri-Spinelli T, Heilmann J, Rali T, et al. Bioactive coumarin derivatives from the fern Cyclosorus interruptus. Planta Med 2000; 66: 728–733.
[29] Valadbeigi E, Ghodsi S. Synthesis and Characterization of Some New Thiazolidinedione Derivatives Containing a Coumarin Moiety for their Antibacterial and Antifungal Activities. Med Chem (Los Angeles) 2017; 07: 178–185.
[30] Abd-El-Aziz AS, El-Agrody AM, Bedair AH, et al. Synthesis of hydroxyquinoline derivatives, amino-hydroxychromene, aminocoumarin and their anti-bacterial activities. Heterocycles 2004; 63: 1793–1812.
[31] Tataringa G, Stan C, Mircea C, et al. Antioxidant evaluation of some coumarin derivatives. Farmacia 2016; 64: 533–538.
[32] Špirtović-Halilović S, Veljović E, Salihović M, et al. Synthesis, microbiological activity and in Silico investigation for some synthesized coumarin derivatives. Croat Chem Acta 2020; 93: 1–9.
[33] Tandel P, Khalifa Z, Upadhyay R, et al. Investigation of recent advancement in the pharmacological potential of C-3 substituted coumarin derivatives against S. aureus. Discov Chem; 2. Epub ahead of print 2025. DOI: 10.1007/s44371-025-00134-x.
[34] Imran M, Khan SA. Synthesis and Antimicrobial Activity of Some 2-Amino-4- ( 7- Substituted / Unsubstituted Coumarin-3-yl ) -6- ( Chlorosubstitutedphenyl ) Pyrimidines. 2015; 14: 1265–1272.
[35] Ahmed R, Al-Shuaeeb A. Synthesis of new coumarin derivatives containing aminobenzotriazole, triazole moieties and their antimicrobial activities. J Med Sci 2023; 1: 1.
[36] Benci K, Mandić L, Suhina T, et al. Novel coumarin derivatives containing 1,2,4-triazole, 4,5-dicyanoimidazole and purine moieties: Synthesis and evaluation of their cytostatic activity. Molecules 2012; 17: 11010–11025.




