full issue - Association of Biotechnology and Pharmacy
full issue - Association of Biotechnology and Pharmacy
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Current Trends in <strong>Biotechnology</strong> <strong>and</strong> <strong>Pharmacy</strong>Vol. 5 (1) 1021-1028 January 2011. ISSN 0973-8916 (Print), 2230-7303 (Online)1028electron releasing groups as seen in the case <strong>of</strong>compound B 15, B 13<strong>and</strong> B 14. This clearly revealsthe importance <strong>of</strong> electron releasing groups onthe aromatic ring in enhancing the antiinflammatoryactivity <strong>and</strong> hence attempts can bemade to synthesize chalcones having a number<strong>of</strong> such electron releasing substituents at differentpositions <strong>of</strong> the aromatic ring as part <strong>of</strong> preparingmore potent compounds.However, the contributing physicochemicalproperties for the anti-inflammatoryactivity <strong>of</strong> the chalcones need to be establishedby detailed QSAR studies, which may provideinsights into the structural requirements <strong>of</strong> thisclass <strong>of</strong> molecules. Further studies are requiredto establish the mechanism <strong>of</strong> anti-inflammatoryactivity <strong>of</strong> these compounds, even though literaturereports suggest the inhibition <strong>of</strong> COX-2 enzymein some cases.ConclusionsChalcones with heterocyclic nucleussuch as indole, pyrrole <strong>and</strong> also the substituentswith electron releasing groups such as methoxy,methyl showed better anti-inflammatory activity.Compounds having pharmacophores such asfluoro, chloro, bromo groups have exhibitedmoderate anti-inflammatory activity. These resultssuggest that’s the chalcone derivatives haveexcellent scope for further development ascommercial anti-inflammatory agents.References1. Bohm, B.A. (1998) In: Introduction toFlavanoids, Harwood Academic Publishers,Amsterdam.2. Kumar, S.K., Hager, E., Pettit, C.,Gurulingappa, H., Davidson, N.E. <strong>and</strong>Khan, S.R. (2003) Design, synthesis <strong>and</strong>evaluation <strong>of</strong> novel boronicchalcone derivativesas antitumor agents. J.Med.Chem., 46:2813.3. Mukarami, S., Muramatsu, M., Aihara, H.<strong>and</strong> Otomo, S. (1991) Inhibition <strong>of</strong> gastricH + , K + -ATPase by the antiulcer agentS<strong>of</strong>alcone. Biochem. Pharmacol., 42: 1447.4. Viana, G.S., B<strong>and</strong>eira, M. A. <strong>and</strong> Matos, F.(2003) Analgesic <strong>and</strong> anti-inflammatory effects<strong>of</strong> chalcones isolated fromMyracrodruonurundeuva.J.Phytomedicine., 10:189.5. Onyilagna, J.C., Malhotra, B., Elder, M. <strong>and</strong>Towers, G.H.N. (1997) Synthesis <strong>and</strong>antimicrobial activity <strong>of</strong> some chalconederivatives. Can.J.Plant Pathol., 19: 133.6. Liu, M., Wilairat, P. <strong>and</strong> Go, L.M (2001)Antimalarial alkoxylated <strong>and</strong> hydroxylatedchalcones: structure-activity relationshipanalysis. J.Med.Chem., 44: 4443.7. Chen, Z-H., Zheng, C-Ji., Sun, L-P. <strong>and</strong> Piao,H-R. (2010) Synthesis <strong>of</strong> new chalconederivatives containing a rhodanine-3-aceticacid moiety with potential antibacterialactivity. Eur. J. Med. Chem., 45: 5739.8. Prasad, Y.R., Kumar, P.R., Deepti, Ch.A.<strong>and</strong> Ramana, M.V. (2007) Synthesis <strong>and</strong>antimicrobial activity <strong>of</strong> some chalcones <strong>of</strong>3-acetylcoumarin <strong>and</strong> 2-hydroxy-1-acetonaphthone.Asian.J.Chem., 19: 4799.9. Prasad, Y.R., Kumar, P.R., Srivani, N. <strong>and</strong>Rao, A.S. (2006) Synthesis <strong>and</strong> antimicrobialactivity <strong>of</strong> some new chalcone derivatives.Int.J.Chem.Sci., 44: 905.10. Turner, R.A. (1965) In: Screening Methodsin Pharmacology, Demic Press, NewYork,p. 152.11. Winter, C.A., Risley, E.A. <strong>and</strong> Nuss, G.W.(1962) Carrageenan induced edema in hindpaw <strong>of</strong> the rat as an assay for anti-inflammatorydrugs. Proc. Soc. Exp. Biol. Med.,111: 544.Srinadh et al