New derivatives of dehydroabietic acid target planktonic and biofilm bacteria in Staphylococcus aureus and effectively disrupt bacterial membrane integrity

Suvi Manner, Mikko Vahermo, Malena Skogman, Sara Krogerus, Pia M. Vuorela, Jari Yli-Kauhaluoma, Adyary Fallarero , Vânia M. Moreira

Tutkimustuotos: ArtikkelijulkaisuArtikkeliTieteellinenvertaisarvioitu

Kuvaus

The combination of the dehydroabietic acid scaffold with different amino acids resulted in the discovery of a new class of hybrid compounds that targets both planktonic and biofilms bacteria in Staphylococcus aureus strains and are far more potent anti-biofilm agents than conventional antibiotics. Unlike dehydroabietic acid, these compounds can disrupt biofilms within a short time period and compromise the integrity of the bacterial membrane. Two of the compounds identified in our study are the most potent abietane-type anti-biofilm agents reported so far and display robust activity against pre-formed biofilms at concentrations only 3-6-fold higher than those required to inhibit biofilm formation. Their easy preparation based on proteolysis-resistant D- and unusual amino acids makes them useful chemical probes to gain a deeper understanding of bacterial biofilms and outstanding candidates for further development into new drugs to fight infections. (C) 2015 Elsevier Masson SAS. All rights reserved.
Alkuperäiskielienglanti
LehtiEuropean Journal of Medicinal Chemistry
Vuosikerta102
Sivut68-79
Sivumäärä12
ISSN0223-5234
DOI - pysyväislinkit
TilaJulkaistu - 21 heinäkuuta 2015
OKM-julkaisutyyppiA1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä, vertaisarvioitu

Tieteenalat

  • 317 Farmasia

Lainaa tätä

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title = "New derivatives of dehydroabietic acid target planktonic and biofilm bacteria in Staphylococcus aureus and effectively disrupt bacterial membrane integrity",
abstract = "The combination of the dehydroabietic acid scaffold with different amino acids resulted in the discovery of a new class of hybrid compounds that targets both planktonic and biofilms bacteria in Staphylococcus aureus strains and are far more potent anti-biofilm agents than conventional antibiotics. Unlike dehydroabietic acid, these compounds can disrupt biofilms within a short time period and compromise the integrity of the bacterial membrane. Two of the compounds identified in our study are the most potent abietane-type anti-biofilm agents reported so far and display robust activity against pre-formed biofilms at concentrations only 3-6-fold higher than those required to inhibit biofilm formation. Their easy preparation based on proteolysis-resistant D- and unusual amino acids makes them useful chemical probes to gain a deeper understanding of bacterial biofilms and outstanding candidates for further development into new drugs to fight infections. (C) 2015 Elsevier Masson SAS. All rights reserved.",
keywords = "317 Pharmacy",
author = "Suvi Manner and Mikko Vahermo and Malena Skogman and Sara Krogerus and Vuorela, {Pia M.} and Jari Yli-Kauhaluoma and Adyary Fallarero and Moreira, {V{\^a}nia M.}",
year = "2015",
month = "7",
day = "21",
doi = "10.1016/j.ejmech.2015.07.038",
language = "English",
volume = "102",
pages = "68--79",
journal = "European Journal of Medicinal Chemistry",
issn = "0223-5234",
publisher = "ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER",

}

New derivatives of dehydroabietic acid target planktonic and biofilm bacteria in Staphylococcus aureus and effectively disrupt bacterial membrane integrity. / Manner, Suvi; Vahermo, Mikko ; Skogman, Malena; Krogerus, Sara; Vuorela, Pia M.; Yli-Kauhaluoma, Jari ; Fallarero , Adyary; Moreira, Vânia M.

julkaisussa: European Journal of Medicinal Chemistry, Vuosikerta 102, 21.07.2015, s. 68-79.

Tutkimustuotos: ArtikkelijulkaisuArtikkeliTieteellinenvertaisarvioitu

TY - JOUR

T1 - New derivatives of dehydroabietic acid target planktonic and biofilm bacteria in Staphylococcus aureus and effectively disrupt bacterial membrane integrity

AU - Manner, Suvi

AU - Vahermo, Mikko

AU - Skogman, Malena

AU - Krogerus, Sara

AU - Vuorela, Pia M.

AU - Yli-Kauhaluoma, Jari

AU - Fallarero , Adyary

AU - Moreira, Vânia M.

PY - 2015/7/21

Y1 - 2015/7/21

N2 - The combination of the dehydroabietic acid scaffold with different amino acids resulted in the discovery of a new class of hybrid compounds that targets both planktonic and biofilms bacteria in Staphylococcus aureus strains and are far more potent anti-biofilm agents than conventional antibiotics. Unlike dehydroabietic acid, these compounds can disrupt biofilms within a short time period and compromise the integrity of the bacterial membrane. Two of the compounds identified in our study are the most potent abietane-type anti-biofilm agents reported so far and display robust activity against pre-formed biofilms at concentrations only 3-6-fold higher than those required to inhibit biofilm formation. Their easy preparation based on proteolysis-resistant D- and unusual amino acids makes them useful chemical probes to gain a deeper understanding of bacterial biofilms and outstanding candidates for further development into new drugs to fight infections. (C) 2015 Elsevier Masson SAS. All rights reserved.

AB - The combination of the dehydroabietic acid scaffold with different amino acids resulted in the discovery of a new class of hybrid compounds that targets both planktonic and biofilms bacteria in Staphylococcus aureus strains and are far more potent anti-biofilm agents than conventional antibiotics. Unlike dehydroabietic acid, these compounds can disrupt biofilms within a short time period and compromise the integrity of the bacterial membrane. Two of the compounds identified in our study are the most potent abietane-type anti-biofilm agents reported so far and display robust activity against pre-formed biofilms at concentrations only 3-6-fold higher than those required to inhibit biofilm formation. Their easy preparation based on proteolysis-resistant D- and unusual amino acids makes them useful chemical probes to gain a deeper understanding of bacterial biofilms and outstanding candidates for further development into new drugs to fight infections. (C) 2015 Elsevier Masson SAS. All rights reserved.

KW - 317 Pharmacy

U2 - 10.1016/j.ejmech.2015.07.038

DO - 10.1016/j.ejmech.2015.07.038

M3 - Article

VL - 102

SP - 68

EP - 79

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

SN - 0223-5234

ER -