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

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 0.5–0.25μM. Compound 12 and SQ109 were potent within a MIC range of 1–0.5μM, whilst compound 18 displayed an activity within the MIC range of 0.5–2μM against both Mycobacterium tuberculosis strains. [Copyright &y& Elsevier]