Synthesis and evaluation of SQ109 analogues as potential anti-tuberculosis candidates
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- 作者：Oluseye K. Onajole ; Patrick Govender ; Paul D. van Helden ; Hendrik G. Kruger ; Glenn E.M. Maguire ; Ian Wiid ; Thavendran Govender
- 关键词：Anti-tuberculosis (TB) ; SQ109 ; 1 ; 2 Cage diamine ; XDR
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2010
- 出版时间：May 2010
- 年：2010
- 卷：45
- 期：5
- 页码：2075-2079
- 全文大小：263 K
文摘
As part of an ongoing project to develop highly potent anti-tuberculosis therapeutics, six SQ109 derivatives were synthesized and screened in vitro for their anti-tuberculosis activity against the ATCC strain H37Rv and the extensively drug-resistant clinical strain XDR 173. Compound 16 with an extended alkene chain was the most active against both strains of Mycobacterium tuberculosis within a MIC range of 0.5–0.25 μM. Compound 12 and SQ109 were potent within a MIC range of 1–0.5 μM, whilst compound 18 displayed an activity within the MIC range of 0.5–2 μM against both Mycobacterium tuberculosis strains.