Saint Petersburg State University, 26 Universitetskii Prospect, 198504 Peterhof, Russia.
Immanuel Kant Baltic Federal University, 236041 Kaliningrad, Russia.
Molecules. 2022 Jun 18;27(12):3910. doi: 10.3390/molecules27123910.
Screening of a library of novel -hydroxylactams amenable by the Castagnoli-Cushman reaction identified four lead compounds that facilitated Fe transport into cells (one of these synthetic siderophores was found to be as efficient at promoting iron uptake as the natural siderophores pyoverdine, pyochelin or enterobactin). Conjugates of the four lead siderophores with ciprofloxacin were tested for antibacterial activity against POA1 (wild type) and the mutant strain. The antibacterial activity was found to be pronounced against the mutant strain grown in CAA medium but not for the POA1 strain. This may be indicative of these compounds being 'Trojan horse' antibiotics. Further scrutiny of the mechanism of the antibacterial action of the newly developed conjugates is warranted.
通过 Castagnoli-Cushman 反应筛选新型 -羟基内酰胺文库，鉴定出了 4 种能促进铁进入细胞的先导化合物（其中一种合成的铁载体与天然铁载体绿脓菌素、焦脱镁叶绿酸或 enterobactin 的铁摄取促进作用一样有效）。将这 4 种先导铁载体与环丙沙星缀合，测试其对 POA1（野生型）和 突变株的抗菌活性。结果发现，这些化合物在 CAA 培养基中对 突变株的抗菌活性显著，但对 POA1 菌株则没有。这可能表明这些化合物是“特洛伊木马”抗生素。值得进一步研究新开发的缀合物的抗菌作用机制。
