full issue - Association of Biotechnology and Pharmacy

Current Trends in Biotechnology and PharmacyVol. 5 (1) 1021-1028 January 2011. ISSN 0973-8916 (Print), 2230-7303 (Online)1028electron releasing groups as seen in the case ofcompound B 15, B 13and B 14. This clearly revealsthe importance of electron releasing groups onthe aromatic ring in enhancing the antiinflammatoryactivity and hence attempts can bemade to synthesize chalcones having a numberof such electron releasing substituents at differentpositions of the aromatic ring as part of preparingmore potent compounds.However, the contributing physicochemicalproperties for the anti-inflammatoryactivity of the chalcones need to be establishedby detailed QSAR studies, which may provideinsights into the structural requirements of thisclass of molecules. Further studies are requiredto establish the mechanism of anti-inflammatoryactivity of these compounds, even though literaturereports suggest the inhibition of COX-2 enzymein some cases.ConclusionsChalcones with heterocyclic nucleussuch as indole, pyrrole and 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. andKhan, S.R. (2003) Design, synthesis andevaluation of novel boronicchalcone derivativesas antitumor agents. J.Med.Chem., 46:2813.3. Mukarami, S., Muramatsu, M., Aihara, H.and Otomo, S. (1991) Inhibition of gastricH + , K + -ATPase by the antiulcer agentSofalcone. Biochem. Pharmacol., 42: 1447.4. Viana, G.S., Bandeira, M. A. and Matos, F.(2003) Analgesic and anti-inflammatory effectsof chalcones isolated fromMyracrodruonurundeuva.J.Phytomedicine., 10:189.5. Onyilagna, J.C., Malhotra, B., Elder, M. andTowers, G.H.N. (1997) Synthesis andantimicrobial activity of some chalconederivatives. Can.J.Plant Pathol., 19: 133.6. Liu, M., Wilairat, P. and Go, L.M (2001)Antimalarial alkoxylated and hydroxylatedchalcones: structure-activity relationshipanalysis. J.Med.Chem., 44: 4443.7. Chen, Z-H., Zheng, C-Ji., Sun, L-P. and Piao,H-R. (2010) Synthesis of 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.and Ramana, M.V. (2007) Synthesis andantimicrobial activity of some chalcones of3-acetylcoumarin and 2-hydroxy-1-acetonaphthone.Asian.J.Chem., 19: 4799.9. Prasad, Y.R., Kumar, P.R., Srivani, N. andRao, A.S. (2006) Synthesis and antimicrobialactivity of 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. and Nuss, G.W.(1962) Carrageenan induced edema in hindpaw of the rat as an assay for anti-inflammatorydrugs. Proc. Soc. Exp. Biol. Med.,111: 544.Srinadh et al