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受自然启发的化合物:丁香酚衍生物对菌株的合成及抗菌药敏试验

Nature-Inspired Compounds: Synthesis and Antibacterial Susceptibility Testing of Eugenol Derivatives against Strains.

作者信息

Carradori Simone, Ammazzalorso Alessandra, Niccolai Sofia, Tanini Damiano, D'Agostino Ilaria, Melfi Francesco, Capperucci Antonella, Grande Rossella, Sisto Francesca

机构信息

Department of Pharmacy, "G. d'Annunzio" University of Chieti-Pescara, Via dei Vestini 31, 66100 Chieti, Italy.

Department of Chemistry "Ugo Schiff", University of Florence, Via della Lastruccia 3-13, 50019 Sesto Fiorentino, Italy.

出版信息

Pharmaceuticals (Basel). 2023 Sep 18;16(9):1317. doi: 10.3390/ph16091317.

Abstract

The antimicrobial properties of one of the most important secondary metabolites, Eugenol (), inspired us to design and synthesize three different series of derivatives enhancing its parent compound's anti- activity. Thus, we prepared semisynthetic derivatives through (A) diazo aryl functionalization, (B) derivatization of the hydroxy group of , and (C) elongation of the allyl radical by incorporating a chalcogen atom. The antibacterial evaluation was performed on the reference NCTC 11637 strain and on three drug-resistant clinical isolates and the minimal inhibitory and bactericidal concentrations (MICs and MBCs) highlight the role of chalcogens in enhancing the antimicrobial activity (less than 4 µg/mL for some compounds) of the scaffold (32-64 µg/mL).

摘要

最重要的次生代谢产物之一丁香酚()的抗菌特性启发我们设计并合成了三个不同系列的衍生物,以增强其母体化合物的抗菌活性。因此,我们通过(A)重氮芳基官能化、(B)丁香酚羟基的衍生化以及(C)通过引入硫族元素原子延长烯丙基自由基,制备了半合成衍生物。对参考NCTC 11637菌株和三种耐药临床分离株进行了抗菌评估,最低抑菌浓度和杀菌浓度(MIC和MBC)突出了硫族元素在增强 支架(32 - 64 µg/mL)抗菌活性(某些化合物低于4 µg/mL)方面的作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/25df/10534785/5f2b6270feb6/pharmaceuticals-16-01317-g001.jpg

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