Marine Natural Products Laboratory, Korea Ocean Research and Development Institute, Ansan, Republic of Korea.
Bioorg Med Chem Lett. 2010 Dec 1;20(23):6882-5. doi: 10.1016/j.bmcl.2010.10.029. Epub 2010 Oct 27.
Guided by the inhibitory activities of indole-containing natural products against isocitrate lyase (ICL) from Candida albicans and sortase A (SrtA) from Staphylococcus aureus, a series of compounds structurally analogous to natural products were synthesized. Eight SrtA inhibitors and an ICL inhibitor having higher activities than the natural products were discovered by screening the enzyme inhibitory activities of synthesized compounds. Among the SrtA inhibitors discovered, six exhibited higher activities than p-hydroxymercuribenzoic acid, which suggests that these compounds have great potential as alternative antibacterial agents.
受含吲哚天然产物对白色念珠菌异柠檬酸裂解酶（ICL）和金黄色葡萄球菌天冬氨酸转肽酶 A（SrtA）抑制活性的启发，我们合成了一系列结构类似的天然产物。通过筛选合成化合物对酶抑制活性的筛选，发现了 8 种 SrtA 抑制剂和一种比天然产物活性更高的 ICL 抑制剂。在所发现的 SrtA 抑制剂中，有 6 种的活性高于对羟基汞苯甲酸，这表明这些化合物具有作为替代抗菌剂的巨大潜力。
