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  • Chem Sci Trans., 2016, 5(3),  pp 579-586  

    DOI:10.7598/cst2016.1232

    Research Article

    Synthesis and Biological Activity of Chalcone Derivatives as Anti - Asthmatics Agents

  • MANUVESH SANGWAN and D P. PATHAK
  • Guru Jambheshwar University of Science and Technology, Hisar, India
    New York State Department of Health, Albany, New York 12202
    Delhi Institute of Pharmaceutical Sciences and Research, New Delhi, 110017, India
  • Abstract

    The objective of this study was to explore novel compounds with benzylideneactophenone moiety, which have potential for anti-asthmatic activity and can be potential candidates for PDE4 inhibitory activity. Seventeen different substituted benzylidene acetophenone and chalcones derivatives have been synthesized by condensing derivatives of benzaldehyde and acetophenone using Claisen ?Schmidt condensation. All the compounds were purified and have been characterized by FTIR and NMR spectroscopy. Among 17 compounds, three compounds were selected for investigation for anti-asthmatic activity. The anti-inflammatory and bronchodilatory activity of the novel products was evaluated by rat paw edema method and tracheal relaxation model. Among these compounds, compound 8 ((2E)-1-(3,4-dichlorophenyl)-3-(3,4-dimethoxyphenyl)-2-propen-1-one ) showed relatively higher anti-inflammatory activity which can be attributed to the substitution of hydrophobic group and 3, 4-dialkoxy groups, compound 8 showed a 59.8% bronchodilatory response when compared to Rolipram (100% response), whereas compounds 17 ((2E)-3-(2-Furyl)-1-(3-hydroxyphenyl)-2-propen-1-one) and 13 ((2E)-3-(4-Ethylphenyl)-1-phenyl-2-propen-1-one) showed marginal activity i.e. 41.43% and 24.35% of the standard drug.

    Keywords

    Benzylideneacetophenone, Chalcone derivatives, Anti-asthmatic activity, PDE4 inhibitors

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