Synthesis, characterization and pharmacological evaluation of chalcones and its derivatives for analgesic activity

https://doi.org/10.53730/ijhs.v6nS1.8453

Authors

  • Geeta Lodhi R.K.D.F. College of Pharmacy, SRK University Bhopal, Madhya Pradesh
  • Amit Nayak R.K.D.F. College of Pharmacy, SRK University Bhopal, Madhya Pradesh

Keywords:

Chalcone, Pyrazolines,1,3,5-trisubstituted pyrazolines, Claisen–Schmidt condensation, Pharmacological evaluation, Analgesic

Abstract

Chalcones have a simple privileged scaffold and are active lead molecules in medicinal chemistry for the discovery of new drugs. Chalcone is the organic compound C6H5C(O)CH=CHC6H5. It is an α, β-unsaturated ketone. Chalcones and their derivatives have a huge importance in medicinal chemistry, displaying a wide range of pharmacological activities including analgesic activites. A variety of important biological compounds are known collectively as chalcones or chalconoids. In this view medicinal chemists are also trying to speed up drug discovery process for finding the lead molecule (Thomas et al. 1998). The compounds with chalcone as backbone have been reported to possess varied biological and pharmacological activities, including antimicrobial, anti-inflammatory, analgesic, cytotoxic, antitumor, antimalarial, antitubercular, antiviral, anti-HIV, antiulcerative, antileishmanial activities.All the newly synthesized pyrimidines were characterized by means of IR, ¹H- and ¹³C-NMR, Electron Ionization (EI)-mass and elemental analyses and screened for analgesic activities. Pyrimidines also displayed better analgesic activity.

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References

Di Carlo, G.; Mascolo, N.; Izzo, A.A.; Capasso, F. Flavonoids: Old and new aspects of a class of natural therapeutic drugs. Life Sci., 1999, 65, 337-353.

Eddarir, S.; Cotelle, N.; Bakkour,Y.; Rolando, C. An efficient synthesis of chalcones based on the Suzuki reaction. Tetrahedron Lett., 2003, 44, 5359-5363.

Furniss, B.S.; Hannaford, A.J.; Rogers, V.; Smith, P.W.G.; Tatchell, A.R. (1989). Vogel’s Textbook of Practical Organic Chemistry, 5th ed.; Longman Group Limited: New York, p. 1034.

Guida, A.; Lhouty, M. H.; Tichit, D.; Figueras, F.; Geneste, P. Hydrotalcites as base catalysts. Kinetics of Claisen-Schmidt condensation, intramolecular condensation of acetonylacetone and synthesis of chalcone. Appl. Catal. A, 1997, 164, 251-264

Kini, S.; Gandhi, A.M. (2008). Novel 2-pyrazoline derivatives as potential antibacterial and antifungal agents. Indian J. Pharm. Sci. 70, 105-108.

Leon, C.; Rodrigues, J.; Dominguez, N.; Rosenthal, P.J.; Dominguez, J.N. (2007). Synthesis and evaluation of sulfonylurea derivatives as novel antimalarials. Eur. J. Med. Chem. 42, 735-742.

Romagnoli, R.; Baraldi, P.G.; Carrion, M.D.; Cruz-Lopez, O.; Cara, C.L.; Balzarini, J.; Hamel, E.; Canella, A.; Fabbri, E.; Gambari, R.; Basso, G.; Viola, G. Hybrid α-bromoacryloylamido chalcones. Design, synthesis and biological evaluation. Bioorganic & Medicinal Chemistry Letters, 2009,19, 2022–2028.

Sonmez, F.; Sevmezler, S.; Atahan, A.; Ceylan, M.; Demir, D.; Gencer, N.; Arslan, O.; Kucukislamoglu, M. (2011). Evaluation of new chalcone derivatives as polyphenol oxidase inhibitors. Bioorg. Med. Chem. Lett. 21, 7479-7482.

Sreedhar NY, MR Jayapal,K Seenivasa Prasad and P Reddy Prasad. Res. J. Pharm Bio. Chemical Sci. 2010; 1(4): 480-484.

Thomas L, David A Willams, Victoria F Roche, Willams S Zito. Foyes Principle of Medicinal chemistry. 6th ed. Newyork: Lippincott publicators; 1998.

Lavie, D. Evaluation of analgesic property of compounds. Lewis Pharmacology. 5 Edn, 461 (1999).

Eddy, N.B. and Leimtach, D. J. Pharmacol. Exp. Ther., 106, 385 (1953).

Published

05-06-2022

How to Cite

Lodhi, G., & Nayak, A. (2022). Synthesis, characterization and pharmacological evaluation of chalcones and its derivatives for analgesic activity. International Journal of Health Sciences, 6(S1), 13665–13678. https://doi.org/10.53730/ijhs.v6nS1.8453

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Peer Review Articles