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

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1TitleTitle of DocumentSynthesis and Biological Activity of Chalcone Derivatives as Anti - Asthmatics Agents
2CreatorAuthor's name, affiliation, country 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
3SubjectDicipline(s) Chemical Science
3SubjectKeywords Benzylideneacetophenone, Chalcone derivatives, Anti-asthmatic activity, PDE4 inhibitors
4DescriptionAbstract 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.
5PublishersOrganizing agency, location WWW Publications, India
6Contributor Sponsor(s) -
7DateDate (YYYY-MM-DD) -
8TypeStatus & genre Peer-reviewed Article
8TypeType
9FormateFile Formate PDF
10IdentifierUniform Resource Identifier Click Here
10IdentifierDigital Object Identifier DOI:10.7598/cst2016.1232
11SourceJournal/conference title; vol., no. (Year)Chemical Science Transactions, Volume  5 , Number  (3), (2016)
12LanuguageEnglish=en en
13RelationSupp.files
14Coverage -
15CopyrightCopyright and permissions
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