Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Eskişehir, Turkey.
J Enzyme Inhib Med Chem. 2013 Aug;28(4):830-5. doi: 10.3109/14756366.2012.688043. Epub 2012 May 31.
In this work, we synthesized fourteen different compounds which contain hydrazone bridged thiazole and pyrrole rings. For this purpose, pyrrole-2-carboxaldehydes were reacted directly with thiosemicarbazide in ethanol and then obtained thiosemicarbazones were condensed with α-bromoacetophenone derivatives (Hantzsch reaction) to give 1-substituted pyrrole-2-carboxaldehyde [4-(4-substituted phenyl)-1,3-thiazol-2-yl] hydrazones. The structures of the obtained compounds were elucidated by using IR, (1)H-NMR and FAB(+)-MS spectral data and elemental analyses results. All of the compounds were screened for their antibacterial and antifungal activities against twelve different microorganisms by using microbroth dilution method. Ketoconazole and chloramphenicol were used as standard drugs. All of the compounds showed good activity against Staphylococcus aureus and Enterococcus faecalis.
在这项工作中，我们合成了 14 种不同的化合物，其中包含腙桥连的噻唑和吡咯环。为此，吡咯-2-甲醛直接与硫代卡巴肼在乙醇中反应，然后得到的硫代卡巴腙与α-溴代苯乙酮衍生物（Hantzsch 反应）缩合，得到 1-取代的吡咯-2-甲醛[4-（4-取代苯基）-1,3-噻唑-2-基]腙。通过使用 IR、(1)H-NMR 和 FAB(+)-MS 光谱数据和元素分析结果阐明了所得化合物的结构。使用微量稀释法对所有化合物进行了针对 12 种不同微生物的抗菌和抗真菌活性筛选。酮康唑和氯霉素被用作标准药物。所有化合物对金黄色葡萄球菌和粪肠球菌均显示出良好的活性。
