DESIGN SYSTHESIS AND EVALUATION OF ANTI BACTERIAL ACTIVITY FOR CHALCONE AND IT’S DERIVATIVE
Keywords:
chalcones, biomolecular interactions, synthesis, natural products, bioactivities, mechanisms, anticancer, antimicrobial, phenolics
Abstract
Chalcones, a subclass of flavonoid-based phenolic compounds, represent one of the most abundant families of bioactive natural products. Their distinctive chemical architecture and broad pharmacological spectrum—including anticancer, anti-inflammatory, antimicrobial, antioxidant, and antiparasitic activities—have sparked significant interest in the synthesis of chalcone derivatives. Owing to their straightforward construction from simple aromatic precursors, chalcones offer a flexible platform for structural modification, enabling the generation of diverse functionalized analogues. These synthetic derivatives often mirror the bioactivity of their natural counterparts, with many exhibiting superior potency and reduced toxicity. This review highlights the potential of bioinspired chalcone synthesis to expand chemical space for drug discovery. Emphasis is placed on evaluating the biological activities of synthesized chalcones and their derivatives, exploring their molecular interactions, and elucidating possible mechanisms of action.
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References
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[5] B-T Kim; K-J O; J-C Chun; K-J Hwang, Bull. Korean Chem. Soc., 2008, 29(6), 1125-1130.
[6] G Yoon; BY Kang; SH Cheon, Arch. Pharm. Res., 2007, 30(3), 313-316.
[7] HD Durst; GW Gokel, Experimental Organic Chemistry., 2nd Edition, McGraw-Hill Publishing Company, New York, 1987, 428-430.
[8] S Sebti; A Solhi; R Tahir; S Boulaajaj; JA Mayoral; JM Fraile; A Kossir; H Oumimoun, Tetrahedron Lett., 2001, 42, 7953-7955.
[9] J Lopez; R Jacquot; F Figueras, Stud. Surf. Sci. Catal., 2000, 130, 491-496.
[10] P Salehi; MM Khodaei; MA Zolfigol; A Keyvan, Monatshefte fuer Chemie., 2002, 133, 1291-1295.
[11] Daud, A.I., et al., Synthesis, spectroscopic, structural elucidation, NLO characteristic and Hirshfeld surface analysis of (E)-1-(4-ethylphenyl)-3-(4-(heptyloxy) phenyl) prop-2-en-1 one: a dual approach of experimental and DFT calculations, Journal of Molecular Structure 1194 (2019) 124-137.
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[14] K Sahu, N., et al., Exploring pharmacological significance of chalcone scaffold: a review, Current medicinal chemistry 19(2) (2012) 209-225.
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[16] Sarafraz, M., et al., 3D-QSAR study on the DYRK1A inhibitors and design of new compounds by CoMFA and CoMSIA methods.
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[18] Mouna, A., et al., Spectroscopic analysis and theoretical comparison of the reactivity of 6-amino-3 (R) benzophenone reactions with acetylacetone, Chemical Review and Letters 7(10) (2024) 942-956.
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[21] Ouyang, Y., et al., Chalcone derivatives: role in anticancer therapy, Biomolecules 11(6) (2021) 894.
[22] Nematollahi, M.H., et al., Antiviral and antimicrobial applications of chalcones and their derivatives: From nature to greener synthesis, Heliyon 9(10) (2023).
[23] Sinha, S., et al., Antimalarial and immunomodulatory potential of chalcone derivatives in experimental model of malaria, BMC Complementary Medicine and Therapies 22(1) (2022) 330.
[24] Garcia, A.R., et al., Identification of chalcone derivatives as inhibitors of Leishmania infantum arginase and promising antileishmanial agents, Frontiers in Chemistry 8 (2021) 624678.
[25] Emam, S.H., et al., Design and synthesis of methoxyphenyl-and coumarin-based chalcone derivatives as anti-inflammatory agents by inhibition of NO production and down-regulation of NF-κB in LPS induced RAW264. 7 macrophage cells, Bioorganic Chemistry 107 (2021) 104630.
[26] N. Bandeira, P., et al., Synthesis, structural characterization, and cytotoxic evaluation of chalcone derivatives, Medicinal Chemistry Research 28 (2019) 2037-2049.
[27] Jin, Q.-H., et al., Synthesis and biological effects of naphthalene-chalcone derivatives, Medicinal Chemistry Research 29 (2020) 877-886.
[28] Okolo, E.N., et al., New chalcone derivatives as potential antimicrobial and antioxidant agent, Scientific reports11(1) (2021) 21781.
[29] Albrecht S, Elpelt A, Kasim C, Reble C, Mundhenk L, Pischon H, et al. Quantification and characterization of radical production in human, animal, and 3D skin models during sun irradiation measured by EPR spectroscopy. Free Radical Biology and Medicine. 2019; 131:299-308
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[35] Austin, M. B., & Noel, J. P. " The chalcone synthase superfamily of type III polyketide synthases." Nat. Prod. Rep. 2003,20,79-110.
[36] Winkel- Shirley, B. "Flavonoid Biosynthesis. A colourful model for genetics, biochemistry, cell biology, and biotechnology." Plant Physiol. 2001,126,485-493.
[37] Dhakhda, K. et al. (2024). Brief Review on Physicochemical Properties of Chalcone, Synthetic Pathway and Analogues with Application. ResearchGate
[38] Singh, P. et al. (2020). Synthesis and Spectral Characterization of Chalcone Derivatives. Journal of Applicable Chemistry, 9(3), 456–462.
[39] Kumar, S. et al. (2021). Chalcones: Chemistry and Therapeutic Potential. Bioorganic Chemistry, 112, 104889.https://doi.org/10.1016/j.bioorg.2021.104889
[40] Patel, K. et al. (2022). Physicochemical and Pharmacokinetic Profiling of Chalcone Derivatives. Chemistry Select, 7(10), e202200123.
[41] Sharma, R. et al. (2019). Qualitative Analysis of Chalcones and Their Derivatives. International Journal of Pharmaceutical Sciences Review and Research, 56(1), 45–50.
[42] Dhakhda, K. et al. (2024). Brief Review on Physicochemical Properties of Chalcone, Synthetic Pathway and Analogues with Application. ResearchGate PDF
[43] Şahin, M. et al. (2022). Chemical and Structural Properties of Chalcones I. FABAD Journal of Pharmaceutical Sciences, 34), 223–242. PDF
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[45] Patel, K. et al. (2022). Physicochemical and Pharmacokinetic Profiling of Chalcone Derivatives. ChemistrySelect, 7(10), e202200123.
[46] Dao, T.T. et al. (2011). Chalcones from Natural Sources and Their Biological Activities. Phytochemistry Reviews, 10(2), 195–206. https://doi.org/10.1007/s11101-010-9181-z
[47] Chalcone Scaffolds, Bio-precursors of Flavonoids: Chemistry, Bioactivities, and Pharmacokinetics Journal: Molecules DOI: 10.3390/molecules26237177
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[49] Batovska D. I.& Todorova I. T., Curr Clin Pharmacol et al. 2010,5(1) :1-29.
[50] Yadav V.R.et al., Phytochem Rev.2011,10:155-172.
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[52] Domínguez J. N.et al., Bio org Med Chem Lett. 2005,15(1) :116-119.
[53] Ahmed A. et al., Front Pharmacol. 2017,8:327.
[54] Ni L. et al., Med Res Rev. 2022,42(3):1124-1184.
[55] Singh P. et al., Arab J Chem.2014 7(6) :1139-1151.
[56] Jain P. et al. J Mol Struct. 2021,1228:129432.
[57] Dixon R. A., Photochemistry. 200156(3):229-243.
[58] Yadav R. et al., J Agric food Chem. 2019,67(15) 4157-4164.
[59] Zhou K, Yang S, Li S-M. Naturally occurring prenylated chalcones from plants: structural diversity, distribution, activities and biosynthesis. Nat Prod Rep. 2021;38(12):2313–2340.
[60] Zhou K, Yang S, Li S-M. Naturally occurring prenylated chalcones from plants: structural diversity, distribution, activities and biosynthesis. Nat Prod Rep. 2021;38(12):2313–2340.
[61] Buckett L, Riedl KM, Schwartz SJ. The pharmacokinetics of individual conjugated xanthohumol metabolites show efficient glucuronidation and higher bioavailability of micellar than native xanthohumol. Mol Nutr Food Res. 2022;66(24):2200684.
[62] Buckett L, Riedl KM, Schwartz SJ. The pharmacokinetics of individual conjugated xanthohumol metabolites show efficient glucuronidation and higher bioavailability of micellar than native xanthohumol. Mol Nutr Food Res. 2022;66(24):2200684.
[63] Zhou K, Yang S, Li S-M. Naturally occurring prenylated chalcones from plants: structural diversity, distribution, activities and biosynthesis. Nat Prod Rep. 2021;38(12):2313–2340.
[64] Oledzka E, Cielecka-Piontek J, Ziemińska E, et al. Xanthohumol—A miracle molecule with biological activities: A review of biodegradable polymeric carriers and naturally derived compounds for its delivery. Int J Mol Sci. 2024;25(6):3398.
[65] Oledzka E, Cielecka-Piontek J, Ziemińska E, et al. Xanthohumol—A miracle molecule with biological activities: A review of biodegradable polymeric carriers and naturally derived compounds for its delivery. Int J Mol Sci. 2024;25(6):3398.
[66] Exploring natural chalcones: innovative extraction techniques, bioactivities, and health potential - Sustainable Food Technology (RSC Publishing)
[67] Chemistry and synthetic methodologies of chalcones and their derivatives: A review
[68] Synthesis of Chalcones Derivatives and Their Biological Activities: A Review | ACS Omega
[69](PDF) Synthesis, Pharmacological Activity and Uses of Chalcone Compounds: A Review
[70] Chalcones—Features, Identification Techniques, Attributes, and Application in Agriculture
[71]IJCSP24A1136.pdf
[72] Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence - PMC
[73]Isolation and biological activity of natural chalcones based on antibacterial mechanism classification - ScienceDirect
[74]8.Laxmiprasanna-Alloli.pdf
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[76] Chalcone - Wikipedia
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[78] Mahapatra et al., 2015 – SAR of chalcones in diabetes therapy
[79] Avial, 2008; Prasad et al., 2007 – Hydroxylation patterns and antioxidant effects
[80] Konduru et al., 2013 – Halogen and methoxy substitutions in antibacterial chalcones
[81] Xu et al., 2019 – Review on antibacterial chalcones and SAR insights
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[83] Avial, 2008; Prasad et al., 2007 – Hydroxylation patterns and antioxidant effects
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Published
2026-03-07
How to Cite
M.Laxmi Priya, K.Teja Rani, K. Suma Sarvani, K.Lavanya, K.L.S.V.N.Sai, & K.M.D.N.S.Sri. (2026). DESIGN SYSTHESIS AND EVALUATION OF ANTI BACTERIAL ACTIVITY FOR CHALCONE AND IT’S DERIVATIVE. IJRDO-Journal of Applied Science, 12(1), 18-38. https://doi.org/10.53555/as.v12i1.6582
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