Carradori Simone, Ammazzalorso Alessandra, Niccolai Sofia, Tanini Damiano, D'Agostino Ilaria, Melfi Francesco, Capperucci Antonella, Grande Rossella, Sisto Francesca
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.
Pharmaceuticals (Basel). 2023 Sep 18;16(9):1317. doi: 10.3390/ph16091317.
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).
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。