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  • Title: Capsaicin derivatives with nitrothiophene substituents: Design, synthesis and antibacterial activity against multidrug-resistant S. aureus.
    Author: Wang ZC, Wei B, Pei FN, Yang T, Tang J, Yang S, Yu LF, Yang CG, Yang F.
    Journal: Eur J Med Chem; 2020 Jul 15; 198():112352. PubMed ID: 32387838.
    Abstract:
    To address the emergency caused by multi-drug resistant Staphylococcus aureus, a series of novel capsaicin derivatives with nitrothiophene substituents have been designed and evaluated for the antibacterial activities against S. aureus Newman and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271). The structure-activity relationship was further revealed. Compound 13c, 13f, and 13g were highly active against staphylococcal growth, with minimal inhibition concentration (MIC) values of 0.39-1.56 μg/mL. The oxadiazole-derived compound 21, a bioisostere of ester 13f, is the most potent candidate for anti-growth of five multidrug-resistant S. aureus strains with MICs of 0.20-0.78 μg/mL, which is more active compared with vancomycin in vitro. Notably, these anti-staphylococcal compounds are much less cytotoxic to the normal kidney epithelial cell line (HK293T).
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