Di-isatin heteronuclear compounds and their antibacterial activity |
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Authors: | Tianwei Ma Rongxing Chen Huarui Xue Zhong Miao Liyan Chen Hao Zhang Xiangkui Shi |
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Institution: | 1. Xuzhou Women & Children's Health Care Hospital, Xuzhou, China;2. Department of Neurosurgery, Second Division, Xuzhou Central Hospital, Xuzhou, 221009 China |
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Abstract: | Twenty propylene and butylene tethered di-isatin heteronuclear compounds 5a-t were synthesized, and their antibacterial activities were evaluated. Most of the synthesized di-isatin heteronuclear derivatives were active against both Gram-positive and Gram-negative strains, and some of them exhibited considerable activities against drug-resistant organisms. In particular, di-isatin 5a (MIC: 32-512 μg/mL) was more active than the reference vancomycin against Gram-negative pathogens, demonstrating the antibacterial potential of di-isatin heteronuclear compounds. The inhibitory activity of di-isatin 5a was higher than mono-isatin against Escherichia coli DNA gyrase, suggesting the dimers could improve the inhibitory activity against DNA gyrase when compared with the isatin. The structure-activity relationship was discussed to provide an insight for rational designs of more efficient antibacterial candidates. |
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