Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, 200241, China.
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
Eur J Med Chem. 2019 Jan 15;162:203-211. doi: 10.1016/j.ejmech.2018.11.016. Epub 2018 Nov 8.
Several 6-substituted tetrahydrocarbazole derivatives were designed, synthesized and evaluated for the antibacterial activities against Staphylococcus aureus Newman strain. Subsequently, 2,4-diaminopyrimidine scaffold was merged with the tetrahydrocarbazole unit to generate a series of novel hybrid derivatives and the antibacterial activities were also investigated. Among these novel hybrids, compound 12c showed the most potent activity with a MIC of 0.39-0.78 μg/mL against S. aureus Newman and Escherichia coli AB1157 strain. In addition, compound 12c exhibited low MIC values against a panel of multidrug-resistant strains of S. aureus.
设计、合成了几种 6-取代四氢咔唑衍生物，并评价了它们对金黄色葡萄球菌 Newman 株的抗菌活性。随后，将 2,4-二氨基嘧啶支架与四氢咔唑单元融合，生成了一系列新型杂合衍生物，并对其抗菌活性进行了研究。在这些新型杂合物中，化合物 12c 对金黄色葡萄球菌 Newman 和大肠杆菌 AB1157 菌株表现出最强的活性，MIC 为 0.39-0.78μg/mL。此外，化合物 12c 对一组耐多药的金黄色葡萄球菌菌株表现出较低的 MIC 值。
