New potent antibacterials against Gram-positive multiresistantpathogens: Effects of side chain modification and chirality inlinezolid-like 1,2,4-oxadiazoles

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

New potent antibacterials against Gram-positive multiresistantpathogens: Effects of side chain modification and chirality inlinezolid-like 1,2,4-oxadiazoles

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

Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche

Risultato della ricerca: Article › peer review

11 Citazioni (Scopus)

Abstract

The effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles have been studiedto design new potent antibacterials against Gram-positive multidrug-resistant pathogens. The adoptedstrategy involved a molecular modelling approach, the synthesis and biological evaluation of newdesigned compounds, enantiomers separation and absolute configuration assignment. Experimentaldetermination 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 resistantlinezolid bacterial strains was higher than that of linezolid.

Lingua originale	English
pagine (da-a)	6819-6825
Numero di pagine	7
Rivista	BIOORGANIC & MEDICINAL CHEMISTRY
Volume	22
Stato di pubblicazione	Published - 2014

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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Palumbo Piccionello, A., Guarcello, A., Pace, A., Lonati, E., Caltabiano, G., Guarcello, A., Pace, A., Bonaccorso, C., Berardozzi, R., Musumarra, G., Pescitelli, G., Pierro, P., Bulbarelli, A., Goracci, L., Fortuna, C. G., Di Bari, L., Cocuzza, C. E. A., Musumeci, R., Palumbo Piccionello, A., & Pierro, P. (2014). New potent antibacterials against Gram-positive multiresistantpathogens: Effects of side chain modification and chirality inlinezolid-like 1,2,4-oxadiazoles. BIOORGANIC & MEDICINAL CHEMISTRY, 22, 6819-6825.

New potent antibacterials against Gram-positive multiresistantpathogens: Effects of side chain modification and chirality inlinezolid-like 1,2,4-oxadiazoles. / Palumbo Piccionello, Antonio ; Guarcello, Annalisa ; Pace, Andrea; Lonati, Elena; Caltabiano, Gianluigi; Guarcello, Annalisa; Pace, Andrea; Bonaccorso, Carmela; Berardozzi, Roberto; Musumarra, Giuseppe; Pescitelli, Gennaro; Pierro, Paola; Bulbarelli, Alessandra; Goracci, Laura; Fortuna, Cosimo G.; Di Bari, Lorenzo; Cocuzza, Clementina E.A.; Musumeci, Rosario; Palumbo Piccionello, Antonio; Pierro, Paola.

In: BIOORGANIC & MEDICINAL CHEMISTRY, Vol. 22, 2014, pag. 6819-6825.

Risultato della ricerca: Article › peer review

Palumbo Piccionello, A , Guarcello, A , Pace, A, Lonati, E, Caltabiano, G, Guarcello, A, Pace, A, Bonaccorso, C, Berardozzi, R, Musumarra, G, Pescitelli, G, Pierro, P, Bulbarelli, A, Goracci, L, Fortuna, CG, Di Bari, L, Cocuzza, CEA, Musumeci, R, Palumbo Piccionello, A & Pierro, P 2014, 'New potent antibacterials against Gram-positive multiresistantpathogens: Effects of side chain modification and chirality inlinezolid-like 1,2,4-oxadiazoles', BIOORGANIC & MEDICINAL CHEMISTRY, vol. 22, pagg. 6819-6825.

Palumbo Piccionello, Antonio ; Guarcello, Annalisa ; Pace, Andrea ; Lonati, Elena ; Caltabiano, Gianluigi ; Guarcello, Annalisa ; Pace, Andrea ; Bonaccorso, Carmela ; Berardozzi, Roberto ; Musumarra, Giuseppe ; Pescitelli, Gennaro ; Pierro, Paola ; Bulbarelli, Alessandra ; Goracci, Laura ; Fortuna, Cosimo G. ; Di Bari, Lorenzo ; Cocuzza, Clementina E.A. ; Musumeci, Rosario ; Palumbo Piccionello, Antonio ; Pierro, Paola. / New potent antibacterials against Gram-positive multiresistantpathogens: Effects of side chain modification and chirality inlinezolid-like 1,2,4-oxadiazoles. In: BIOORGANIC & MEDICINAL CHEMISTRY. 2014 ; Vol. 22. pagg. 6819-6825.

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title = "New potent antibacterials against Gram-positive multiresistantpathogens: Effects of side chain modification and chirality inlinezolid-like 1,2,4-oxadiazoles",

abstract = "The effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles have been studiedto design new potent antibacterials against Gram-positive multidrug-resistant pathogens. The adoptedstrategy involved a molecular modelling approach, the synthesis and biological evaluation of newdesigned compounds, enantiomers separation and absolute configuration assignment. Experimentaldetermination 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 resistantlinezolid bacterial strains was higher than that of linezolid.",

author = "{Palumbo Piccionello}, Antonio and Annalisa Guarcello and Andrea Pace and Elena Lonati and Gianluigi Caltabiano and Annalisa Guarcello and Andrea Pace and Carmela Bonaccorso and Roberto Berardozzi and Giuseppe Musumarra and Gennaro Pescitelli and Paola Pierro and Alessandra Bulbarelli and Laura Goracci and Fortuna, {Cosimo G.} and {Di Bari}, Lorenzo and Cocuzza, {Clementina E.A.} and Rosario Musumeci and {Palumbo Piccionello}, Antonio and Paola Pierro",

year = "2014",

language = "English",

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pages = "6819--6825",

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T1 - New potent antibacterials against Gram-positive multiresistantpathogens: Effects of side chain modification and chirality inlinezolid-like 1,2,4-oxadiazoles

AU - Palumbo Piccionello, Antonio

AU - Guarcello, Annalisa

AU - Pace, Andrea

AU - Lonati, Elena

AU - Caltabiano, Gianluigi

AU - Guarcello, Annalisa

AU - Pace, Andrea

AU - Bonaccorso, Carmela

AU - Berardozzi, Roberto

AU - Musumarra, Giuseppe

AU - Pescitelli, Gennaro

AU - Pierro, Paola

AU - Bulbarelli, Alessandra

AU - Goracci, Laura

AU - Fortuna, Cosimo G.

AU - Di Bari, Lorenzo

AU - Cocuzza, Clementina E.A.

AU - Musumeci, Rosario

AU - Palumbo Piccionello, Antonio

AU - Pierro, Paola

PY - 2014

Y1 - 2014

N2 - The effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles have been studiedto design new potent antibacterials against Gram-positive multidrug-resistant pathogens. The adoptedstrategy involved a molecular modelling approach, the synthesis and biological evaluation of newdesigned compounds, enantiomers separation and absolute configuration assignment. Experimentaldetermination 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 resistantlinezolid bacterial strains was higher than that of linezolid.

AB - The effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles have been studiedto design new potent antibacterials against Gram-positive multidrug-resistant pathogens. The adoptedstrategy involved a molecular modelling approach, the synthesis and biological evaluation of newdesigned compounds, enantiomers separation and absolute configuration assignment. Experimentaldetermination 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 resistantlinezolid bacterial strains was higher than that of linezolid.

UR - http://hdl.handle.net/10447/103056

M3 - Article

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SP - 6819

EP - 6825

JO - BIOORGANIC & MEDICINAL CHEMISTRY

JF - BIOORGANIC & MEDICINAL CHEMISTRY

SN - 0968-0896

ER -