Document Details
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Document Type |
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Article In Journal |
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Document Title |
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Synthesis and Biological Evaluation of some 2,4,5-Trisubstituted Thiazole Derivatives as Potential A Synthesis and Biological Evaluation of some 2,4,5-Trisubstituted Thiazole Derivatives as Potential A |
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Document Language |
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English |
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Abstract |
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We wish to report on the synthesis and biological evaluation of two series of 2,4,5-polysubstituted thiazoles comprising the acid hydrazide functionality and some derived pharmacophores such as the imino, ureido, thioureido, sulfonamido, N-formyl, N-acetyl, semicarbazide and thiosemicarbazide that are reported to contribute to various chemotherapeutic activities. All the newly synthesized compounds have been subjected to in vitro antibacterial and antifungal screening. Out of the compounds tested, 22 derivatives displayed distinctive inhibitory effect on the growth of the tested Gram positive strains while they lack activity against Gram negative bacteria. Moreover, 12 compounds were able to exert antifungal activity against C. albicans. Potential antibacterial and antifungal activities were linked to the thiosemicarbazide function 6a-f and those substituted with both the thioureido and thiosemicarbazide moieties 12a-f. Compounds 6f and 12f (R = 4-F-C6H4) could be considered as the most active members in the present investigation with a potential broad spectrum antibacterial activity against the three types of Gram positive bacteria tested, together with an appreciable antifungal activity against C. albicans. Compounds 6d, 6f and 12f were twice as active as ampicillin against B. subtilis. The best antifungal activity was shown by compound 6d which was 50% less active than clotrimazole. On the other hand, 17 compounds were selected and tested for their preliminary in vitro anticancer activity according to the current one-dose protocol of the NCI. Three cell lines namely; the non-small cell lung cancer Hop-92, ovarian cancer IGROV1 and melanoma SK-MEL-2 exhibited pronounced sensitivity against most of the tested 17 compounds. Compound 12f proved to be the most active anticancer member in this study with a broad spectrum of activity against most of the |
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ISSN |
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0365-6233 |
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Journal Name |
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WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim |
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Volume |
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341 |
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Issue Number |
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7 |
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Publishing Year |
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2008 AH
1428 AD |
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Article Type |
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Article |
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Added Date |
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Tuesday, April 8, 2008 |
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Researchers
| Mohammed Al-Saadi | Al-Saadi, Mohammed | Researcher | Doctorate | hfaidallah@hotmail.com |
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Files
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34270.pdf
| pdf | Synthesis and Biological Evaluation of Some 2,4,5-Trisubstituted Thiazole Derivatives as Potential Antimicrobial and Anticancer Agents |
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