A New Kind of Quinonic-Antibiotic Useful Against Multidrug-Resistant S. aureus and E. faecium Infections

Javier Campanini-Salinas, Juan Andrades-Lagos, Gerardo Gonzalez Rocha, Duane Choquesillo-Lazarte, Soledad Bollo Dragnic, Mario Faúndez, Pedro Alarcón, Francisco Silva, Roberto Vidal, Edison Salas-Huenuleo, Marcelo Kogan, Jaime Mella, Gonzalo Recabarren Gajardo, David Vásquez-Velásquez

Resultado de la investigación: Article

1 Cita (Scopus)

Resumen

A rapid emergence of resistant bacteria is occurring worldwide, endangering the efficacy of antibiotics and reducing the therapeutic arsenal available for treatment of infectious diseases. In the present study, we developed a new class of compounds with antibacterial activity obtained by a simple, two step synthesis and screened the products for in vitro antibacterial activity against ATCC® strains using the broth microdilution method. The compounds exhibited minimum inhibitory concentrations (MIC) of 1⁻32 μg/mL against Gram-positive ATCC® strains. The structure⁻activity relationship indicated that the thiophenol ring is essential for antibacterial activity and the substituents on the thiophenol ring module, for antibacterial activity. The most promising compounds detected by screening were tested against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VREF) clinical isolates. We found remarkable activity against VREF for compounds 7 and 16, were the MIC50/90 were 2/4 µg/mL and 4/4 µg/mL, respectively, while for vancomycin the MIC50/90 was 256/512 µg/mL. Neither compound affected cell viability in any of the mammalian cell lines at any of the concentrations tested. These in vitro data show that compounds 7 and 16 have an interesting potential to be developed as new antibacterial drugs against infections caused by VREF.

Idioma originalEnglish
PublicaciónMolecules (Basel, Switzerland)
Volumen23
N.º7
DOI
EstadoPublished - 19 jul 2018
Publicado de forma externa

Huella dactilar

Enterococcus faecium
antibiotics
infectious diseases
Vancomycin
Anti-Bacterial Agents
Infection
Cells
Microbial Sensitivity Tests
Methicillin-Resistant Staphylococcus aureus
Arsenals
Methicillin
Communicable Diseases
broths
Cell Survival
staphylococcus
rings
Bacteria
Cell Line
Screening
cultured cells

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

Citar esto

Campanini-Salinas, J., Andrades-Lagos, J., Gonzalez Rocha, G., Choquesillo-Lazarte, D., Bollo Dragnic, S., Faúndez, M., ... Vásquez-Velásquez, D. (2018). A New Kind of Quinonic-Antibiotic Useful Against Multidrug-Resistant S. aureus and E. faecium Infections. Molecules (Basel, Switzerland), 23(7). https://doi.org/10.3390/molecules23071776
Campanini-Salinas, Javier ; Andrades-Lagos, Juan ; Gonzalez Rocha, Gerardo ; Choquesillo-Lazarte, Duane ; Bollo Dragnic, Soledad ; Faúndez, Mario ; Alarcón, Pedro ; Silva, Francisco ; Vidal, Roberto ; Salas-Huenuleo, Edison ; Kogan, Marcelo ; Mella, Jaime ; Recabarren Gajardo, Gonzalo ; Vásquez-Velásquez, David. / A New Kind of Quinonic-Antibiotic Useful Against Multidrug-Resistant S. aureus and E. faecium Infections. En: Molecules (Basel, Switzerland). 2018 ; Vol. 23, N.º 7.
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title = "A New Kind of Quinonic-Antibiotic Useful Against Multidrug-Resistant S. aureus and E. faecium Infections",
abstract = "A rapid emergence of resistant bacteria is occurring worldwide, endangering the efficacy of antibiotics and reducing the therapeutic arsenal available for treatment of infectious diseases. In the present study, we developed a new class of compounds with antibacterial activity obtained by a simple, two step synthesis and screened the products for in vitro antibacterial activity against ATCC{\circledR} strains using the broth microdilution method. The compounds exhibited minimum inhibitory concentrations (MIC) of 1⁻32 μg/mL against Gram-positive ATCC{\circledR} strains. The structure⁻activity relationship indicated that the thiophenol ring is essential for antibacterial activity and the substituents on the thiophenol ring module, for antibacterial activity. The most promising compounds detected by screening were tested against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VREF) clinical isolates. We found remarkable activity against VREF for compounds 7 and 16, were the MIC50/90 were 2/4 µg/mL and 4/4 µg/mL, respectively, while for vancomycin the MIC50/90 was 256/512 µg/mL. Neither compound affected cell viability in any of the mammalian cell lines at any of the concentrations tested. These in vitro data show that compounds 7 and 16 have an interesting potential to be developed as new antibacterial drugs against infections caused by VREF.",
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author = "Javier Campanini-Salinas and Juan Andrades-Lagos and {Gonzalez Rocha}, Gerardo and Duane Choquesillo-Lazarte and {Bollo Dragnic}, Soledad and Mario Fa{\'u}ndez and Pedro Alarc{\'o}n and Francisco Silva and Roberto Vidal and Edison Salas-Huenuleo and Marcelo Kogan and Jaime Mella and {Recabarren Gajardo}, Gonzalo and David V{\'a}squez-Vel{\'a}squez",
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Campanini-Salinas, J, Andrades-Lagos, J, Gonzalez Rocha, G, Choquesillo-Lazarte, D, Bollo Dragnic, S, Faúndez, M, Alarcón, P, Silva, F, Vidal, R, Salas-Huenuleo, E, Kogan, M, Mella, J, Recabarren Gajardo, G & Vásquez-Velásquez, D 2018, 'A New Kind of Quinonic-Antibiotic Useful Against Multidrug-Resistant S. aureus and E. faecium Infections', Molecules (Basel, Switzerland), vol. 23, n.º 7. https://doi.org/10.3390/molecules23071776

A New Kind of Quinonic-Antibiotic Useful Against Multidrug-Resistant S. aureus and E. faecium Infections. / Campanini-Salinas, Javier; Andrades-Lagos, Juan; Gonzalez Rocha, Gerardo; Choquesillo-Lazarte, Duane; Bollo Dragnic, Soledad; Faúndez, Mario; Alarcón, Pedro; Silva, Francisco; Vidal, Roberto; Salas-Huenuleo, Edison; Kogan, Marcelo; Mella, Jaime; Recabarren Gajardo, Gonzalo; Vásquez-Velásquez, David.

En: Molecules (Basel, Switzerland), Vol. 23, N.º 7, 19.07.2018.

Resultado de la investigación: Article

TY - JOUR

T1 - A New Kind of Quinonic-Antibiotic Useful Against Multidrug-Resistant S. aureus and E. faecium Infections

AU - Campanini-Salinas, Javier

AU - Andrades-Lagos, Juan

AU - Gonzalez Rocha, Gerardo

AU - Choquesillo-Lazarte, Duane

AU - Bollo Dragnic, Soledad

AU - Faúndez, Mario

AU - Alarcón, Pedro

AU - Silva, Francisco

AU - Vidal, Roberto

AU - Salas-Huenuleo, Edison

AU - Kogan, Marcelo

AU - Mella, Jaime

AU - Recabarren Gajardo, Gonzalo

AU - Vásquez-Velásquez, David

PY - 2018/7/19

Y1 - 2018/7/19

N2 - A rapid emergence of resistant bacteria is occurring worldwide, endangering the efficacy of antibiotics and reducing the therapeutic arsenal available for treatment of infectious diseases. In the present study, we developed a new class of compounds with antibacterial activity obtained by a simple, two step synthesis and screened the products for in vitro antibacterial activity against ATCC® strains using the broth microdilution method. The compounds exhibited minimum inhibitory concentrations (MIC) of 1⁻32 μg/mL against Gram-positive ATCC® strains. The structure⁻activity relationship indicated that the thiophenol ring is essential for antibacterial activity and the substituents on the thiophenol ring module, for antibacterial activity. The most promising compounds detected by screening were tested against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VREF) clinical isolates. We found remarkable activity against VREF for compounds 7 and 16, were the MIC50/90 were 2/4 µg/mL and 4/4 µg/mL, respectively, while for vancomycin the MIC50/90 was 256/512 µg/mL. Neither compound affected cell viability in any of the mammalian cell lines at any of the concentrations tested. These in vitro data show that compounds 7 and 16 have an interesting potential to be developed as new antibacterial drugs against infections caused by VREF.

AB - A rapid emergence of resistant bacteria is occurring worldwide, endangering the efficacy of antibiotics and reducing the therapeutic arsenal available for treatment of infectious diseases. In the present study, we developed a new class of compounds with antibacterial activity obtained by a simple, two step synthesis and screened the products for in vitro antibacterial activity against ATCC® strains using the broth microdilution method. The compounds exhibited minimum inhibitory concentrations (MIC) of 1⁻32 μg/mL against Gram-positive ATCC® strains. The structure⁻activity relationship indicated that the thiophenol ring is essential for antibacterial activity and the substituents on the thiophenol ring module, for antibacterial activity. The most promising compounds detected by screening were tested against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VREF) clinical isolates. We found remarkable activity against VREF for compounds 7 and 16, were the MIC50/90 were 2/4 µg/mL and 4/4 µg/mL, respectively, while for vancomycin the MIC50/90 was 256/512 µg/mL. Neither compound affected cell viability in any of the mammalian cell lines at any of the concentrations tested. These in vitro data show that compounds 7 and 16 have an interesting potential to be developed as new antibacterial drugs against infections caused by VREF.

KW - antibacterial activity

KW - methicillin-resistant Staphylococcus aureus

KW - quinonic-antibiotics

KW - vancomycin-resistant Enterococcus faecium

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U2 - 10.3390/molecules23071776

DO - 10.3390/molecules23071776

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JO - Molecules

JF - Molecules

SN - 1420-3049

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Campanini-Salinas J, Andrades-Lagos J, Gonzalez Rocha G, Choquesillo-Lazarte D, Bollo Dragnic S, Faúndez M y otros. A New Kind of Quinonic-Antibiotic Useful Against Multidrug-Resistant S. aureus and E. faecium Infections. Molecules (Basel, Switzerland). 2018 jul 19;23(7). https://doi.org/10.3390/molecules23071776