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The semi-synthesis, biological evaluation and docking analysis of the oxime, hydrazine and hydrazide derivatives of platensimycin†
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2018-03-06 00:00:00 , DOI: 10.1039/c8md00081f
Youchao Deng 1 , Dingding Kang 1 , Jie Shi 1 , Wenqing Zhou 1 , Aijun Sun 2 , Jianhua Ju 2 , Xiangcheng Zhu 1, 3 , Ben Shen 1, 4 , Yanwen Duan 1, 3, 5 , Yong Huang 1, 5
Affiliation  

A dozen oxime, hydrazine and hydrazide derivatives of platensimycin (PTM) analogues were synthesized, some of which showed strong antibacterial activities and were shown to be stable under the bioassay conditions. Docking analysis revealed that they have certain new interactions with β-ketoacyl-[acyl carrier protein] synthase II (FabF), suggesting that Schiff base formation on its terpene scaffold is an effective strategy to diversify PTM structure.

中文翻译:

平板霉素肟、肼及酰肼衍生物的半合成、生物学评价及对接分析†

合成了十几种平板霉素 (PTM) 类似物的肟、肼和酰肼衍生物,其中一些具有很强的抗菌活性,并且在生物测定条件下表现出稳定。对接分析表明,它们与β-酮酰基-[酰基载体蛋白]合酶II(FabF)具有一定的新相互作用,表明在其萜烯支架上形成席夫碱是使PTM结构多样化的有效策略。
更新日期:2018-03-06
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