School of Chemistry, University of KwaZulu-Natal, Durban, South Africa.
Eur J Med Chem. 2010 May;45(5):2075-9. doi: 10.1016/j.ejmech.2010.01.046. Epub 2010 Jan 28.
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.
作为开发高效抗结核治疗药物的持续项目的一部分，合成了六个 SQ109 衍生物，并对其体外抗结核活性进行了筛选，以对抗 ATCC 株 H37Rv 和广泛耐药的临床株 XDR173。具有延长烯链的化合物 16 对两种结核分枝杆菌菌株的 MIC 范围为 0.5-0.25μM 时最具活性。化合物 12 和 SQ109 在 MIC 范围 1-0.5μM 时具有很强的活性，而化合物 18 对两种结核分枝杆菌菌株的 MIC 范围为 0.5-2μM 时显示出活性。
