Synthesis, Characterization And Microbial Activity Of New Thiazole, Thiazolidinone, Thiadiazole And Phenylacrylohydrazide Substituted Coumarin Derivatives
| dc.contributor.author | Yusuf Zai, Samina Khan | |
| dc.date.accessioned | 2017-01-09T07:56:16Z | |
| dc.date.available | 2017-01-09T07:56:16Z | |
| dc.date.issued | 2015-07 | |
| dc.description.abstract | Thiazoles, thiazolidinones, thiadiazoles, phenylacrylohydrazides and coumarins, are few of the very important classes of heterocyclic compounds having great medicinal and pharmacological importance. In the present study, six series of 67 new biologically active coumarin derived compounds have been synthesized by substituting thiazole, thiazolidinone, thiadiazole and phenylacrylohydrazide units into the coumarin core, in order to increase their use as important therapeutic agents. The structures of all the new compounds were characterized by spectroscopic techniques such as, IR, 1D NMR (1H and 13C) and CHN analysis together with LCMS. The structures of the selective compounds from each series were further confirmed by 2D NMR (COSY, HMQC and HMBC) spectroscopic techniques. In addition to this X-Ray diffraction analysis was used to confirm, the structures for those compounds obtained as single crystals. The structures of all the synthesized starting materials were confirmed by the comparison of their spectroscopic data with those already reported in literature. Melting point measurements was done for all the synthesized compounds, in order to check their purity. All the synthesized coumarin analogues were screened in vitro for their antibacterial activity against two Grampositive bacteria Streptococcus pneumoniae and Staphylococcus aureus and three Gram-negative bacteria Escherichia coli, Enterobacter aerogenes and Salmonella typhi, including Mycobacterium tuberculosis, a bacterium which causes tuberculosis disease. Significant activity against Mycobacterium tuberculosis was shown by almost all the compounds. Strongest inhibition was shown by the halogenated compound 29g with the lowest MIC value of 60.0 M, while its analogue 29f and the other coumarins 27b, 30a and 26 also revealed good activities with MIC values of 83, λ3, 83 and λ3 M, respectively as compared to that of the control drug, Isoniazid. Moreover, in antibacterial activity the strongest inhibition against the aforementioned bacteria strains were observed again by the group of halogenated compounds (27b, 28b, 28i, 28p, 29d, 29h, 30b, 31b, and 32d), with MIC values ranging from 34 to 233 M as compared to those of the standard drugs streptomycin, kanamycin and vancomycin. Rest other coumarin derivatives were also found to exhibit significant anti bacterial activities. The results of this study concluded the potential uses of coumarin derived compounds, in medicine and drug discovery. | en_US |
| dc.identifier.uri | http://hdl.handle.net/123456789/3366 | |
| dc.subject | Chemistry | en_US |
| dc.title | Synthesis, Characterization And Microbial Activity Of New Thiazole, Thiazolidinone, Thiadiazole And Phenylacrylohydrazide Substituted Coumarin Derivatives | en_US |
| dc.type | Thesis | en_US |
Files
License bundle
1 - 1 of 1
Loading...
- Name:
- license.txt
- Size:
- 1.71 KB
- Format:
- Item-specific license agreed upon to submission
- Description: