期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 10, 页码 2866-2868出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.03.082
关键词
Ferrocene; Quinoline; Ferroquine; Antibacterial; Antitubercular activity
资金
- South African Research Chairs Initiative of the Department of Science and Technology administered through South African National Research Foundation
- South African Medical Research Council
- University of Cape Town
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 mu g/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 mu g/ml) against M. tuberculosis. This new drug may offer an interesting alternative in endemic area where malaria and tuberculosis coexist. (C) 2011 Elsevier Ltd. All rights reserved.
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