Antibacterial and Synergistic Activity of a New 8-Hydroxyquinoline Derivative Against Methicillin-Resistant Staphylococcus Aureus

Abstract

Aim: To evaluate the antibacterial and synergistic effect of a new 8-hydroxyquinoline derivative (PH176) against MRSA. Materials & methods: PH176 activity was determined by broth microdilution against 38 Staphylococcus aureus clinical isolates. The antibacterial and synergistic effects with oxacillin and nitroxoline were evaluated by time–kill assays to five MRSA isolates. Toxicity was evaluated by in vitro and ex vivo models. Results: The MIC50 and MIC90 of PH176 were 16 and 32 μg/ml, respectively. The PH176 and nitroxoline led to a reduction in colony count for four isolates and the combination of PH176 and oxacillin acted synergically for three isolates. Furthermore, PH176 was determined to be noncytotoxic/nonirritant. Conclusion: These results demonstrate that PH176 has revealed promising results to be a potential candidate to treat MRSA infections.

Chemopreventive Effect on Human Colon Adenocarcinoma Cells of Styrylquinolines: Synthesis, Cytotoxicity, Proapoptotic Effect and Molecular Docking Analysis

“…Its antitumor effect has mainly been associated with its ability to modulate oxidative stress, inflammation, platelet aggregation, and the induction of tumor cell apoptosis [ 11 , 12 , 13 ]. On the other hand, 8-hydroxyquinoline is a heterocyclic organic compound known to be a chelating agent with antimicrobial and anticancer activity [ 14 , 15 , 16 , 17 ]. Specifically, its anticancer activity has been associated with its possible ability to inhibit the proliferation and migration of cancer cells through the induction of apoptosis and the generation of ROS, among other mechanisms [ 18 , 19 , 20 ].…”

PhI(OAc)2/Pd(OAc)2 promoted the formation of 8-hydroxyquinoline derivatives from benzoxazoles and alcohols

“…1,2 Historically, 8-HQ has played an important role in agriculture and textile, wood, and paper industries. 3,4 Moreover, functionalized 8-HQs are widely used to detect various metal ions and anions in organic chemistry and analytical chemistry because of their good metal recognition properties. 4–6 In the past two decades, owing to the remarkable biological activities of 8-hydroxyquinoline derivatives, such as anti-cancer, 7,8 antibacterial, 3,9 antifungal, 10 anti-HIV 11 and neuroprotective activities, 12,13 8-hydroxyquinoline derivatives have attracted continuous attention from medicinal chemists.…”

“…3,4 Moreover, functionalized 8-HQs are widely used to detect various metal ions and anions in organic chemistry and analytical chemistry because of their good metal recognition properties. 4–6 In the past two decades, owing to the remarkable biological activities of 8-hydroxyquinoline derivatives, such as anti-cancer, 7,8 antibacterial, 3,9 antifungal, 10 anti-HIV 11 and neuroprotective activities, 12,13 8-hydroxyquinoline derivatives have attracted continuous attention from medicinal chemists. 14,15 Driven by the significance of this skeleton, chemists have devoted great efforts to explore efficient synthetic methods to access 8-hydroxyquinoline derivatives.…”