作者:Kenton J. Hetrick、Miguel A. Aguilar Ramos、Ronald T. Raines
DOI:10.1021/acschembio.0c00894
日期:2021.5.21
ant bacteria, new strategies to expand the repertoire of antimicrobial compounds are necessary. Prodrugs are an underexploited strategy in this effort. Here, we report on the enhanced antimicrobial activity of a prodrug toward bacteria having an enzyme capable of its activation. A screen led us to the sulfurol ester of the antibiotic trans-3-(4-chlorobenzoyl)acrylic acid. An endogenous esterase makes
鉴于抗微生物细菌的持续威胁,有必要采用新的策略来扩大抗微生物化合物的种类。在这项工作中,前药是一种未充分利用的策略。在这里,我们报告了前药对具有能够激活其的酶的细菌的增强的抗菌活性。通过筛选,我们发现了抗生素反式-3-(4-氯苯甲酰基)丙烯酸的硫醇酯。内源性酯酶使耻垢分枝杆菌对该前药敏感。候选酯酶被鉴定,它们的异源生产使大肠杆菌对酯类前药敏感。综上所述,这些数据提出了一种开发抗微生物化合物的新方法,该方法利用内源性酶活性来靶向特定细菌。