扁枝衣霉素肟、肼及酰肼衍生物的半合成、生物学评价及对接分析
The semi-synthesis, biological evaluation and docking analysis of the oxime, hydrazine and hydrazide derivatives of platensimycin.
作者信息
Deng Youchao, Kang Dingding, Shi Jie, Zhou Wenqing, Sun Aijun, Ju Jianhua, Zhu Xiangcheng, Shen Ben, Duan Yanwen, Huang Yong
机构信息
Xiangya International Academy of Translational Medicine at Central South University , Changsha , Hunan 410013 , China . Email:
CAS Key Laboratory of Tropical Marine Bio-resources and Ecology , Guangdong Key Laboratory of Marine Materia Medica , RNAM Center for Marine Microbiology , South China Sea Institute of Oceanology , Chinese Academy of Sciences , 164 West Xingang Road , Guangzhou 510301 , China.
出版信息
Medchemcomm. 2018 Mar 6;9(5):789-794. doi: 10.1039/c8md00081f. eCollection 2018 May 1.
Abstract
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.
摘要
合成了十二种扁枝衣霉素（PTM）类似物的肟、肼和酰肼衍生物，其中一些表现出较强的抗菌活性，并且在生物测定条件下显示稳定。对接分析表明，它们与β-酮酰基-[酰基载体蛋白]合酶II（FabF）有某些新的相互作用，这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。
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