oxadiazoles has been researched along with Peritonitis* in 3 studies
1 review(s) available for oxadiazoles and Peritonitis
| Article | Year |
|---|---|
The oxadiazole antibacterials.
The oxadiazoles are a class of antibacterials discovered by in silico docking and scoring of compounds against the X-ray structure of a penicillin-binding protein. These antibacterials exhibit activity against Gram-positive bacteria, including against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE). They show in vivo efficacy in murine models of peritonitis/sepsis and neutropenic thigh MRSA infection. They are bactericidal and orally bioavailable. The oxadiazoles show promise in treatment of MRSA infection. Topics: Animals; Anti-Bacterial Agents; beta-Lactams; Female; Methicillin-Resistant Staphylococcus aureus; Mice; Mice, Inbred ICR; Microbial Sensitivity Tests; Oxadiazoles; Peritonitis; Quantitative Structure-Activity Relationship; Staphylococcal Infections; Vancomycin-Resistant Enterococci | 2016 |
2 other study(ies) available for oxadiazoles and Peritonitis
| Article | Year |
|---|---|
Structure-based screening for the discovery of 1,2,4-oxadiazoles as promising hits for the development of new anti-inflammatory agents interfering with eicosanoid biosynthesis pathways.
The multiple inhibition of biological targets involved in pro-inflammatory eicosanoid biosynthesis represents an innovative strategy for treating inflammatory disorders in light of higher efficacy and safety. Herein, following a multidisciplinary protocol involving virtual combinatorial screening, chemical synthesis, and in vitro and in vivo validation of the biological activities, we report the identification of 1,2,4-oxadiazole-based eicosanoid biosynthesis multi-target inhibitors. The multidisciplinary scientific approach led to the identification of three 1,2,4-oxadiazole hits (compounds 1, 2 and 5), all endowed with IC Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Arachidonate 5-Lipoxygenase; Cell Line; Cell Survival; Cyclooxygenase 1; Dose-Response Relationship, Drug; Drug Development; Drug Evaluation, Preclinical; Eicosanoids; Enzyme Inhibitors; Humans; Male; Mice; Molecular Structure; Oxadiazoles; Peritonitis; Prostaglandin-E Synthases; Structure-Activity Relationship; Zymosan | 2021 |
The Specific Mitogen- and Stress-Activated Protein Kinase MSK1 Inhibitor SB-747651A Modulates Chemokine-Induced Neutrophil Recruitment.
Mitogen-activated protein kinase (MAPK) signaling is involved in a variety of cellular functions. MAPK-dependent functions rely on phosphorylation of target proteins such as mitogen- and stress-activated protein kinase 1 (MSK1). MSK1 participates in the early gene expression and in the production of pro- and anti-inflammatory cytokines. However, the role of MSK1 in neutrophil recruitment remains elusive. Here, we show that chemokine macrophage inflammatory protein-2 (CXCL2) enhances neutrophil MSK1 expression. Using intravital microscopy and time-lapsed video analysis of cremasteric microvasculature in mice, we studied the effect of pharmacological suppression of MSK1 by SB-747651A on CXCL2-elicited neutrophil recruitment. SB-747651A treatment enhanced CXCL2-induced neutrophil adhesion while temporally attenuating neutrophil emigration. CXCL2-induced intraluminal crawling was reduced following SB-747651A treatment. Fluorescence-activated cell sorting analysis of integrin expression revealed that SB-747651A treatment attenuated neutrophil integrin α Topics: Animals; Biomarkers; Bridged Bicyclo Compounds, Heterocyclic; Cell Tracking; Chemokines; Chemotaxis, Leukocyte; Immunophenotyping; Male; Mice; Neutrophils; Oxadiazoles; Peritonitis; Protein Kinase Inhibitors | 2017 |