Biological Activities of Chalcones

Abstract

Chalcone natural or synthetic and chalcone derivatives have exhibited different types of biological activities. Chalcone is widely available in nature and due to its broad spectrum of biological activities, this moiety is often used in molecular design strategies. In this article I have summarised literature evidence on biological activities of chalcone derivatives.

Introduction

The text provides a comprehensive review of chalcones, a class of naturally occurring compounds that serve as key precursors in flavonoid biosynthesis and possess wide-ranging biological and pharmacological activities. Chalcones are biosynthesized via the shikimate pathway and are structurally characterized as 1,3-diaryl propenones. Beyond their chemical importance, chalcones and their derivatives exhibit diverse bioactivities, including antibacterial, antileishmanial, antifungal, antiviral, anti-inflammatory, antimalarial, and antifilarial effects, as well as enzyme inhibition relevant to cellular metabolism.

The review highlights extensive antibacterial activity of chalcones, particularly oxygenated and lipophilic derivatives such as licochalcone A, which show strong bactericidal or bacteriostatic effects depending on substitution patterns. Structure–activity relationship (SAR) studies emphasize the role of lipophilicity, hydroxyl groups, and specific ring substitutions in determining potency. Chalcones also demonstrate notable antileishmanial activity by targeting parasite mitochondrial enzymes, leading to impaired respiration and parasite death.

Antifungal activity is mainly observed against dermatophytes, with electron-withdrawing substituents enhancing potency, while steric effects influence activity. Several chalcone derivatives exhibit antiviral properties, including inhibition of HIV replication, where methoxy substitutions play a critical role. Anti-inflammatory effects are attributed to the inhibition of nitric oxide and prostaglandin E? production through suppression of inducible nitric oxide synthase and cyclooxygenase-2 pathways.

Additionally, chalcones show antifilarial activity by inhibiting glutathione-S-transferase in parasites, resulting in reduced viability and parasite death. Overall, the text underscores the therapeutic potential of chalcones and their derivatives, demonstrating how structural modifications significantly influence biological activity and supporting their continued exploration as promising lead compounds in drug discovery.

Conclusion

This article has summarized different biological activities of natural and synthetic chalcone like anti-filarial, anti-inflammatory, antiviral, antileishmanial, antifungal and antibacterial activity. Their importance stems from this broad bioactivity and ease of synthesis are a driving force for researchers to synthesize new derivatives of chalcone for therapeutic applications. Researchers can modify the chalcone scaffold to develop potent drug candidate specially by incorporating heterocyclic ring (N,O,S) to enhance activity against specific disease targets.

References

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