Department of Chemistry and Institute of Infectious Disease & Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa.
Bioorg Med Chem Lett. 2011 May 15;21(10):2866-8. doi: 10.1016/j.bmcl.2011.03.082. Epub 2011 Mar 30.
We report here the synthesis and in vitro antitubercular activity of a new series of ferrocenyl derivatives. The quinoline-ferrocene hybrid 5 exhibited significant activity (MIC=2.5-5 μg/ml) against Mycobacterium tuberculosis. Results indicate that such hybrid compounds provide an efficient approach for future pharmacological developments to fight against tuberculosis. Moreover, the antimalarial drug candidate ferroquine (FQ, SSR97193) was also evaluated mainly because of its structural similarity. FQ was found to display moderate inhibitory activity (MIC=10-15 μg/ml) against M. tuberculosis. This new drug may offer an interesting alternative in endemic area where malaria and tuberculosis coexist.
我们在此报告了一系列新型二茂铁衍生物的合成及其体外抗结核活性。喹啉-二茂铁杂合物 5 表现出显著的活性（MIC=2.5-5μg/ml），对结核分枝杆菌具有活性。结果表明，此类杂合物为未来的抗结核药理学发展提供了一种有效的方法。此外，还评估了抗疟药物候选药物 ferroquine（FQ，SSR97193），主要是因为其结构相似。FQ 对结核分枝杆菌的抑制活性中等（MIC=10-15μg/ml）。在疟疾和结核病共存的流行地区，这种新药可能提供一种有趣的选择。
