A new class of phenylhydrazinylidene derivatives as inhibitors of Staphylococcus aureus biofilm formation
| العنوان: | A new class of phenylhydrazinylidene derivatives as inhibitors of Staphylococcus aureus biofilm formation |
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| المؤلفون: | Maria Grazia Cusimano, Benedetta Maggio, Ainars Leonchiks, Giuseppe Daidone, Barbara Manachini, Stella Cascioferro, Maria Valeria Raimondi, Demetrio Raffa, Domenico Schillaci |
| المساهمون: | Cascioferro, S., Maggio, B., Raffa, D., Raimondi, M., Cusimano, M., Schillaci, D., Manachini, B., Leonchiks, A., Daidone, G. |
| المصدر: | Medicinal Chemistry Research. 25:870-878 |
| بيانات النشر: | Springer Science and Business Media LLC, 2016. |
| سنة النشر: | 2016 |
| مصطلحات موضوعية: | 0301 basic medicine, medicine.drug_class, 030106 microbiology, Antibiotics, Bacterial adhesion, Antibiofilm agent, Settore BIO/19 - Microbiologia Generale, medicine.disease_cause, Microbiology, Antivirulence agent, 03 medical and health sciences, Antibiotic resistance, In vivo, medicine, General Pharmacology, Toxicology and Pharmaceutics, biology, Chemistry, Sortase A, Organic Chemistry, Biofilm, Phenylhydrazinylidene derivative, biochemical phenomena, metabolism, and nutrition, biology.organism_classification, Settore CHIM/08 - Chimica Farmaceutica, Galleria mellonella, Settore AGR/11 - Entomologia Generale E Applicata, 030104 developmental biology, Mechanism of action, Biochemistry, Staphylococcus aureus, Pharmacology, Toxicology and Pharmaceutics (all), medicine.symptom |
| الوصف: | In the struggle against the emergence of the antibiotic resistance, new molecules targeting biofilm formation could be useful as adjuvant of conventional antibiotics. This study focused on a new class of 2-phenylhydrazinylidene derivatives as antivirulence agents. The compound 12e showed interesting activities against biofilm formation of all tested Staphylococcus aureus strains with IC50 ranging from 1.7 to 43 µM; compounds 12f and 13a resulted strong inhibitors of S. aureus ATCC 6538 and ATCC 29213 biofilm formation with IC50 of 0.9 and 0.8 µM, respectively. A preliminary study on the mechanism of action was carried on evaluating the inhibition of sortase A transpeptidase. Compound 12e resulted not to be toxic at 1 mg/ml by using an in vivo model (the wax moth larva model, Galleria mellonella). |
| تدمد: | 1554-8120 1054-2523 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c04987c18aefb748fb7eb3ae62a700c3Test https://doi.org/10.1007/s00044-016-1535-9Test |
| حقوق: | CLOSED |
| رقم الانضمام: | edsair.doi.dedup.....c04987c18aefb748fb7eb3ae62a700c3 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 15548120 10542523 |
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