Mutai Peggoty, Pavadai Elumalai, Wiid Ian, Ngwane Andile, Baker Bienyameen, Chibale Kelly
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
DST-NRF Centre of Excellence for Biomedical Tuberculosis Research, SAMRC Centre for Tuberculosis Research, Division of Molecular Biology and Human Genetics, Faculty of Medicine and Health Sciences, Stellenbosch University, PO Box 19063, Tygerberg 7505, South Africa.
Bioorg Med Chem Lett. 2015 Jun 15;25(12):2510-3. doi: 10.1016/j.bmcl.2015.04.064. Epub 2015 Apr 28.
The synthesis and antimycobacterial activity of formononetin analogues is hereby reported. Formononetin and its analogue 11E showed 88% and 95% growth inhibition, respectively, against the H37Rv strain of Mycobacterium tuberculosis. Pharmacophore modeling studies indicated that the presence of a hydroxyl group in formononetin and its analogues, is crucial for maintaining activity.
本文报道了刺芒柄花素类似物的合成及其抗分枝杆菌活性。刺芒柄花素及其类似物11E对结核分枝杆菌H37Rv菌株的生长抑制率分别为88%和95%。药效团模型研究表明，刺芒柄花素及其类似物中羟基的存在对维持活性至关重要。
