Journal articles
Search for new tools to combat Gram-negative resistant bacteria among amine derivatives of 5-arylidenehydantoin
Abstract : A series of amine-alkyl derivatives of 5-arylidenehydantoin 3–21 was evaluated for their ability to improve antibiotic effectiveness in two strains of Gram-negative Enterobacter aerogenes: the reference strain (ATCC-13048) and the chloramphenicol-resistant derivative over-producing the AcrAB-TolC efflux pump (CM-64). Three antibiotics, chloramphenicol, nalidixic acid and sparfloxacin were used as markers of efflux pump activity. New compounds (5–16) were obtained within 3–4 step synthesis using Knoevenagel condensation, Mitsunobu reaction and microwave aided N-alkylation. Molecular modeling based structure–activity relationship (SAR) studies were performed. The most active compounds: (Z)-5-(4-(diethylamino)benzylidene)-3-(2-hydroxy-3-(4-(2-hydroxyethyl)piperazin-1-yl)propyl)imidaz-olidine-2,4-dione (14) and (Z)-5-(2,4-dimethoxybenzylidene)-3-(2-hydroxy-3-(isopropylamino)pro-pyl)imidazolidine-2,4-dione (15) induced fourfold decrease of minimal inhibition concentration (MIC) of all tested antibiotics in the strain CM-64 overexpressing the AcrAB-TolC pump.
Cited literature [13 references]
https://hal-amu.archives-ouvertes.fr/hal-01425050
Contributor : Sandrine Alibert <>
Submitted on : Monday, January 16, 2017 - 9:15:31 AM
Last modification on : Thursday, June 20, 2019 - 9:52:06 AM
Long-term archiving on: : Monday, April 17, 2017 - 2:32:26 PM
Contributor : Sandrine Alibert <>
Submitted on : Monday, January 16, 2017 - 9:15:31 AM
Last modification on : Thursday, June 20, 2019 - 9:52:06 AM
Long-term archiving on: : Monday, April 17, 2017 - 2:32:26 PM
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BioorgMedChem2013(21).pdf
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