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

OK Onajole, P Govender, PD van Helden…

Index: Onajole, Oluseye K.; Govender, Patrick; Helden, Paul D. van; Kruger, Hendrik G.; Maguire, Glenn E.M.; Wiid, Ian; Govender, Thavendran European Journal of Medicinal Chemistry, 2010 , vol. 45, # 5 p. 2075 - 2079

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Citation Number: 36

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 μM. Compound 12 and ...