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. 2010 May;45(5):2075-9.
doi: 10.1016/j.ejmech.2010.01.046. Epub 2010 Jan 28.

Synthesis and evaluation of SQ109 analogues as potential anti-tuberculosis candidates

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Synthesis and evaluation of SQ109 analogues as potential anti-tuberculosis candidates

Oluseye K Onajole et al. Eur J Med Chem. 2010 May.

Abstract

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 microM. Compound 12 and SQ109 were potent within a MIC range of 1-0.5 microM, whilst compound 18 displayed an activity within the MIC range of 0.5-2 microM against both Mycobacterium tuberculosis strains.

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