With antibiotics resistance developing rapidly, new antibacterial agents are needed to be discovered. We readily synthesized 11 indolin-2-one compounds and found a hybrid of indolin-2-one and nitroimidazole 3-((1-methyl-5-nitro-1H-imidazol-2-yl)methylene)indolin-2-one to be effective on Staphylococcus aureus strains. Six derivatives of this compound were further designed and synthesized in order to enhance its efficacy. After a second turn of structural refinement, a novel hybrid of indolin-2-one and nitroimidazole 3-((1-methyl-5-nitro-1H-imidazol-2-yl)methylene)-5-nitroindolin-2-one with a nitro group on C-5 position of indolin-2-one was shown to exhibit remarkable antibacterial activities with a low MIC value against MRSA ATCC 33591. Besides, this molecule demonstrated its potency on Gram-negative bacteria and VRE strain. The time-killing curve experiment showed its good bactericidal activity. Low hemolytic rate suggested its promising safety profile.

中文翻译：

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发现吲哚啉-2-一和硝基咪唑的杂种作为抗药性细菌的有效抑制剂。

随着对抗生素的耐药性迅速发展，需要发现新的抗菌剂。我们很容易地合成了11种吲哚啉-2-酮化合物，并发现了吲哚啉-2-酮和硝基咪唑3-（（（1-甲基-5-硝基-1H-咪唑-2-基）亚甲基）吲哚-2-酮的混合物对金黄色葡萄球菌菌株有效。为了增强其功效，进一步设计和合成了该化合物的六种衍生物。经过第二轮结构优化后，吲哚-2-酮和硝基咪唑3-（（（1-甲基-5-硝基-1H-咪唑-2-基）亚甲基）-5-硝基吲哚-2-酮吲哚-2-酮C-5位的硝基显示出显着的抗菌活性，对MRSA ATCC 33591的MIC值低。此外，该分子还显示出对革兰氏阴性菌和VRE菌株的效力。时间杀灭曲线实验表明其具有良好的杀菌活性。低溶血率提示其安全性前景良好。