Search

Your search keyword '"Cocuzza, Cea"' showing total 3 results
Start Over Author "Cocuzza, Cea"
3 results on '"Cocuzza, Cea"'

2. New potent antibacterials against Gram-positive multiresistant pathogens: effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles

Author

Elena Lonati, Alessandra Bulbarelli, Carmela Bonaccorso, Rosario Musumeci, Andrea Pace, Laura Goracci, Roberto Berardozzi, Annalisa Guarcello, Lorenzo Di Bari, Paola Pierro, Cosimo G. Fortuna, Antonio Palumbo Piccionello, Gianluigi Caltabiano, Gennaro Pescitelli, Giuseppe Musumarra, Clementina Cocuzza, Fortuna, CG, Berardozzi, R, Bonaccorso, C, Caltabiano, G, Di Bari, L, Goracci, L, Guarcello, A, Pace, A, Palumbo Piccionello, A, Pescitelli, G, Pierro, P, Lonati, E, Bulbarelli, A, Cocuzza, CEA, Musumarra, G, Musumeci, R, Fortuna, C, and Cocuzza, C

Subjects
Multidrug-resistant bacteria, Clinical Biochemistry, Antibiotics, Drug Resistance, Molecular Conformation, Pharmaceutical Science, Biochemistry, chemistry.chemical_compound, Drug Resistance, Multiple, Bacterial, Drug Discovery, Acetamides, Side chain, Oxadiazoles, Absolute configuration, Bacterial, Stereoisomerism, Hep G2 Cells, BIO/10 - BIOCHIMICA, 23S, Anti-Bacterial Agents, Molecular Docking Simulation, RNA, Ribosomal, 23S, Drug design, Linezolid, Antibiotics, Multidrug-resistant bacteria, Enantiomers, Molecular Medicine, Antibacterial activity, Multiple, Methicillin-Resistant Staphylococcus aureus, Staphylococcus aureus, medicine.drug_class, Stereochemistry, Cell Survival, Microbial Sensitivity Tests, Gram-Positive Bacteria, Drug design, medicine, Humans, Molecular Biology, Oxazolidinones, Ribosomal, Binding Sites, Organic Chemistry, Antibiotic, Linezolid, Settore CHIM/06 - Chimica Organica, Settore CHIM/08 - Chimica Farmaceutica, Multiple drug resistance, chemistry, Enantiomers, MED/07 - MICROBIOLOGIA E MICROBIOLOGIA CLINICA, RNA, Nucleic Acid Conformation, Enantiomer, Chirality (chemistry)
Abstract

The effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles have been studied to design new potent antibacterials against Gram-positive multidrug-resistant pathogens. The adopted strategy involved a molecular modelling approach, the synthesis and biological evaluation of new designed compounds, enantiomers separation and absolute configuration assignment. Experimental determination of the antibacterial activity of the designed (S)-1-((3-(4-(3-methyl-1,2,4-oxadiazol-5- yl)phenyl)-oxazolidin-2-one-5-yl)methyl)-3-methylthiourea and (S)-1-((3-(3-fluoro-4-(3-methyl-1,2,4- oxadiazol-5-yl)phenyl)-oxazolidin-2-one-5-yl)methyl)-3-methylthiourea against multidrug resistant linezolid bacterial strains was higher than that of linezolid.

Published
2014

3. New linezolid-like 1,2,4-oxadiazoles active against Gram-positive multiresistant pathogens

Author

Carmela Bonaccorso, Laura Rizzi, Paola Pierro, Cosimo G. Fortuna, Gianluigi Caltabiano, Giuseppe Musumarra, Clementina Cocuzza, Laura Goracci, Rosario Musumeci, Alessandra Bulbarelli, Annalisa Guarcello, Antonio Palumbo Piccionello, Andrea Pace, Fortuna, C, Bonaccorso, C, Bulbarelli, A, Caltabiano, G, Rizzi, L, Goracci, L, Musumarra, G, Pace, A, Palumbo Piccionello, A, Guarcello, A, Pierro, P, Cocuzza, C, Musumeci, R, Fortuna, CG, and Cocuzza, CEA

Subjects
Methicillin-Resistant Staphylococcus aureus, Models, Molecular, Cell viability, Staphylococcus aureus, Molecular model, Cell Survival, Microbial Sensitivity Tests, Antimicrobial activity, Crystallography, X-Ray, medicine.disease_cause, Drug design, Microbiology, Structure-Activity Relationship, chemistry.chemical_compound, oxadiazoles, linezolid, antibiotics, Cell Line, Tumor, Drug Resistance, Multiple, Bacterial, Morpholine, Acetamides, Drug Discovery, medicine, Humans, Moiety, Structure–activity relationship, Oxazolidinones, Pharmacology, Oxadiazoles, Linezolid, Dose-Response Relationship, Drug, Molecular Structure, Chemistry, Organic Chemistry, Settore CHIM/06 - Chimica Organica, Hep G2 Cells, General Medicine, biochemical phenomena, metabolism, and nutrition, bacterial infections and mycoses, Settore CHIM/08 - Chimica Farmaceutica, Methicillin-resistant Staphylococcus aureus, Combinatorial chemistry, Oxazolidinone, Anti-Bacterial Agents, MED/07 - MICROBIOLOGIA E MICROBIOLOGIA CLINICA, Antibacterial activity, Software
Abstract

The synthesis and the in vitro antibacterial activity of novel linezolid-like oxadiazoles are reported. Replacement of the linezolid morpholine C-ring with 1,2,4-oxadiazole results in an antibacterial activity against Staphylococcus aureus both methicillin-susceptible and methicillin-resistant comparable or even superior to that of linezolid. While acetamidomethyl or thioacetoamidomethyl moieties in the C(5) side-chain are required, fluorination of the phenyl B ring exhibits a slight effect on an antibacterial activity but its presence seems to reduce the compounds cytotoxicity. Molecular modeling performed using two different approaches - FLAP and Amber software - shows that in the binding pose of the newly synthesized compounds as compared with the crystallographic pose of linezolid, the 1,2,4-oxadiazole moiety seems to perfectly mimic the function of the morpholinic ring, since the H-bond interaction with U2585 is retained.

Published
2013

Catalog

Books, media, physical & digital resources
See catalog results