Synthesis and antibacterial activity of pyranmycin derivatives with N-1 and O-6 modifications.
Synthesis and antibacterial activity of pyranmycin derivatives with N-1 and O-6 modifications.
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N-1和O-6修饰吡喃霉素衍生物的合成及其抗菌活性。
DOI：
10.1016/j.bmc.2007.08.059
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发表时间：
2007
影响因子：
3.5
通讯作者：
Chang,Cheng-WeiTom
中科院分区：
文献类型：
--
作者：
Li,Jie;Chiang,Fang-I;Chen,Hsiao-Nung;Chang,Cheng-WeiTom
在我们为对抗耐药细菌而对氨基糖苷类抗生素进行修饰的持续努力的基础上，我们进一步衍生化了吡喃霉素，一种新的氨基糖苷类抗生素，并在O-6和N-1位进行了修改。结果表明，在O-6位，不同的酰基对吡霉素类药物的抗菌活性有一定的调节作用。在这些结果中，6-O-氨基乙基衍生物JT050对耐药菌株大肠杆菌(pTZ19U-3)和大肠杆菌(PSF815)表现出有效的活性，这为进一步的结构修饰提供了线索。
Continuing from our ongoing effort in modifying aminoglycoside antibiotics with the goal of counteracting drug resistant bacteria, we have further derivatized pyranmycin, a neomycin class aminoglycoside antibiotic, with modifications at O-6 and N-1 positions. The revealed SAR results demonstrated that the antibacterial activity of pyranmycin can be modulated by different acylic substituents at O-6. Among these results, the 6-O-aminoethyl derivative, JT050, showed effective activity against resistant strain Escherichia coli (pTZ19U-3) and E. coli (pSF815), which provides insight into further structural modifications.