Gnana Sahaya Jeyanthi, T (2018) Studies on Synthesis, Characterization and Invitro Anti-Inflammatory Activity of Methoxydibenzofuran-1,3-Thiazole- Carboxamide Derivatives. Masters thesis, J.K.K.Nattraja College of Pharmacy, Komarapalayam.
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Abstract
The present work entitled “studies on synthesis, characterization and biological activity methoxydibenzofuran-1, 3-thiazole carboxamide derivatives”, has described the synthesis of ten compounds. It is well established that the presence of dibenzofuranthiazole in molecules has resulted in pharmacologically and biologically active agents these are having a varied type of heterocyclic or otherwise, straight chain structures. Many of the existing drugs, for example, Tetomilast, oglemilast and ciliomilast are potent anti-inflammatory agents, they do have serious side effects. These include nausea, emesis and gastric acid secretion. Many other standard drugs of today also, have other types of unwanted effects one important being drug resistance. Thus, newer agents with out such undesirable side effects and better potency are the need of the day. This work, thus, was undertaken to study a few new compounds. Based on the literature survey tetomilast a PDE inhibitor from otsuka contain thiazole moiety in it and oglemilast contain a new series of dibenzofuran nucleus, also the cilomilast carrying aryl derivatives with the conclusion in mind we forwarded to synthesis dibenzofuran thiazole carboxamide derivatives. All the compounds were prepared in the laboratory and purified by crystallization with suitable solvents. Furthermore, all the structures of the compounds were confirmed by melting point, FTIR, 1H-NMR and High resolution Mass spectroscopy. The cyclic nucleotide phosphodiesterase are a family of enzyme that selectively catalyse the hydrolysis of cAMP and cGMP. The inhibition of the PDEs in the cell effectively elevates the intracellular cAMP level. This in turn inhibits the release of inflammatory mediators (TNF-α, interleukin-2, interleukin -12) and act as a anti inflammatory drug. (Banerjee M et al 2011) In view of that we focused the biological evaluation for all the synthesized compounds. The results of short term in vitro anti-inflammatory screening against protein denaturation method show a moderate inhibitory effect. Among these particularly compounds 4c, 4d, 4e, 4f, 4g and 4h showed promising activity when compared to standard drug diclofenac sodium at lowest concentration of 100 μg/ml and the percentage of inhibition are found to be 26.70, 35.86, 27.16, 27.60, 38.54 and 32.57 μg/ml respectively. Where the standard drug diclofenac sodium was 25.31 μg/ml. Particularly the compound 4d shows a very good inhibiting property at all concentrations (100 -1000μg/ml) when compared to the standard drug. This experiment suggest that the anti-inlammatory activity of dibenzofuranthiazole carboxamide derivatives mainly due to the halogenic derivative with para substitution. The fluro, chloro substitution was one of the key groups to enhance greatly the activity with para and ortho substituent, as well as the methoxy derivatives with meta substituent also shows moderate activity.
| Item Type: | Thesis (Masters) |
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| Additional Information: | REG.No.261615203 |
| Uncontrolled Keywords: | Methoxydibenzofuran-1 ; 3-Thiazole- Carboxamide Derivatives ; Synthesis ; Characterization ; Invitro Anti-Inflammatory Activity. |
| Subjects: | PHARMACY > Pharmaceutical Chemistry |
| Depositing User: | Subramani R |
| Date Deposited: | 28 Jun 2019 02:24 |
| Last Modified: | 28 Jun 2019 02:24 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/10634 |
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