Novel phenolic antimicrobials enhanced activity of iminodiacetate prodrugs against biofilm and planktonic bacteria.,Chemical Biology & Drug Design

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Novel phenolic antimicrobials enhanced activity of iminodiacetate prodrugs against biofilm and planktonic bacteria.
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2020-08-26 , DOI: 10.1111/cbdd.13768
Danica J Walsh _{1,

2} , Tom Livinghouse ₁ , Greg M Durling ₁ , Adrienne D Arnold _{2,

3} , Whitney Brasier ₂ , Luke Berry ₁ , Darla M Goeres ₂ , Philip S Stewart ₂

Affiliation

Prodrugs are pharmacologically attenuated derivatives of drugs that undergo bioconversion into the active compound once reaching the targeted site, thereby maximizing their efficiency. This strategy has been implemented in pharmaceuticals to overcome obstacles related to absorption, distribution, and metabolism, as well as with intracellular dyes to ensure concentration within cells. In this study, we provide the first examples of a prodrug strategy that can be applied to simple phenolic antimicrobials to increase their potency against mature biofilms. The addition of (acetoxy)methyl iminodiacetate groups increases the otherwise modest potency of simple phenols. Biofilm‐forming bacteria exhibit a heightened tolerance toward antimicrobial agents, thereby accentuating the need for new antibiotics as well as those, which incorporate novel delivery strategies to enhance activity toward biofilms.

中文翻译：

新型酚类抗菌剂增强了亚氨基二乙酸酯前药对抗生物膜和浮游细菌的活性。

前药是药物的药理学减毒衍生物，一旦到达靶位点，它们就会生物转化为活性化合物，从而最大限度地发挥其功效。该策略已在药物中实施，以克服与吸收、分布和代谢相关的障碍，以及细胞内染料以确保细胞内的浓度。在这项研究中，我们提供了第一个前药策略的例子，该策略可应用于简单的酚类抗菌剂，以提高其对抗成熟生物膜的效力。 (乙酰氧基)甲基亚氨基二乙酸酯基团的添加增加了简单酚的原本有限的效力。形成生物膜的细菌对抗菌剂表现出更高的耐受性，从而强调了对新型抗生素以及那些结合新的递送策略以增强对生物膜活性的抗生素的需求。

更新日期：2020-08-26

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