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SYNTHESIS, SPECTRAL CHARACTERIZATION OF DIBENZOFURAN-1,3-THIAZOLE CARBOXAMIDE DERIVATIVES AND EVALUATED FOR ANTI-INFLAMMATORY POTENTIAL

Vinit Mishra, Alok Pal Jain, Amit Nayak*


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    "description": "<p><strong><em>Objective:</em></strong><em> The objective of the paper is synthesis and characterization of dibenzofuran-1,3-thiazole carboxamide derivatives and screened for anti-inflammatory potential</em></p>\n\n<p><strong><em>Material and methods:</em></strong><em> The present work was aimed to synthesis some dibenzofuran-1,3 thiazole carboxamide derivatives by four step reactions with the substitution of various substituted benzylamine under suitable catalyst. The compound 1 (S-((4-chlorodibenzo[b,d]furan-1-yl)methyl)thiohydroxylamine), Compound 2 (ethyl 2-(4-chlorodibenzo[b,d]furan-1-yl)-5-methylthiazole-4-carboxylate), compound 3 (2-(4-chlorodibenzo[b,d]furan-1-yl)-5-methylthiazole-4-carboxylic acid) and compound 4 (N-benzyl-2-(4-chlorodibenzo[b,d]furan-1-yl)-5-methyl thiazole-4-carboxamide) were prepared. The Compound 4 coded as compound TC-1 to TC-14. In this four steps process total 12 compounds have been synthesized and evaluated for the anti-inflammatory potential by protein denaturation assay.</em></p>\n\n<p><strong><em>Result and Discussion:</em></strong><em> &nbsp;The IR spectrum of the compounds has shown the characteristics peak (cm<sup>-1</sup>) of</em><em> N-H at 3412; C=C-H at 3470; C=O at 1735; C=C at 1624&ndash;1446; C-N at 1015; </em><em>p-substitution at </em><em>792</em><em>; C-F at 1102</em><strong><em>; </em></strong><em>C-Cl at 855; C-Br at 1015; </em><em>N-O at 1356; N=O at 1558. The 1HNMR spectra of Final compounds (TC-1 to TC-12) depicted the peak at </em><em>2.90 (3H, CH<sub>3</sub>); 4.64 - 4.65 (2H, CH<sub>2</sub>); 7.05-7.10 (2H, Ar-H); 7.35 (1H, Ar-H); 7.33 &ndash; 7.39 (4H, Ar-H); 7.45 (1H, Ar-H); 7.48 - 7.50 (1H, Ar-H); 7.62 - 7.63 (1H, Ar-H); 7.90 - 7.92 (1H, Ar-H); 8.38 &ndash; 8.40 (1H, N-H).</em><em> Compound TC-1, mass spectrum has shown peak at m/z = 450.85, which matches the chemical formula C<sub>24</sub>H<sub>16</sub>ClFN<sub>2</sub>O<sub>2</sub>S. The protein denaturation assay of synthesized compound stated that most active compound are TC-1, TC-2, TC-3, TC-4 and TC-5 and compounds TC-7 &amp; TC-9 has shown the mild activity and compound TC-6, TC-8, TC-10, TC-11 and TC-12 has shown modest activity.&nbsp; </em></p>\n\n<p><strong><em>Conclusion</em></strong><em>: The </em><em>Cl, Br, I, NO<sub>2</sub> and F substitution enhance the activity when it attached to 4-position of the thiazole ring with addition of electronegative atom also enhance the anti-inflammatory potential of compounds</em><em>.</em></p>\n\n<p><strong>Keywords</strong>: <em>Anti-inflammatory, thiazole, protein denaturation assay, dibenzofuran</em></p>", 
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    "title": "SYNTHESIS, SPECTRAL CHARACTERIZATION OF DIBENZOFURAN-1,3-THIAZOLE CARBOXAMIDE DERIVATIVES AND EVALUATED FOR ANTI-INFLAMMATORY POTENTIAL", 
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