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Semi-synthesis of antibacterial dialkylresorcinol derivatives.
The Journal of Antibiotics ( IF 2.1 ) Pub Date : 2020-08-11 , DOI: 10.1038/s41429-020-0359-5
Jianye Li 1 , Yue Shi 1 , Benjamin R Clark 1
Affiliation  

Dialkylresorcinols are a class of antimicrobial natural products produced by a range of bacterial species. Semi-synthetic derivatization of two microbial dialkylresorcinols isolated from a Pseudomonas aurantiaca strain has yielded 21 derivatives, which were tested for antimicrobial activity, revealing several trends in their activity. The presence of aromatic and phenolic hydrogen atoms was crucial for activity, with all derivatives lacking these features possessing greatly reduced activity. On the other hand, derivatives with shorter alkyl chains at C-5 possessed lower MIC values, while one mono-fluorosulfated derivative showed significantly improved activity against several of the test strains.



中文翻译:

抗菌性二烷基间苯二酚衍生物的半合成。

二烷基间苯二酚是由多种细菌产生的一类抗菌天然产物。从aseantimonus aurantiaca菌株中分离出的两种微生物二烷基间苯二酚的半合成衍生化反应产生了21种衍生物,并对其抗微生物活性进行了测试,揭示了其活性的几种趋势。芳族和酚氢原子的存在对于活性至关重要,所有缺乏这些特征的衍生物都具有大大降低的活性。另一方面,在C-5处具有较短烷基链的衍生物具有较低的MIC值,而一种单氟代硫酸化衍生物显示出对几种测试菌株的显着改善的活性。

更新日期:2020-08-11
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