Reference : Pegylated triarylmethanes: Synthesis, antimicrobial activity, anti-proliferative beha...
Scientific journals : Article
Human health sciences : Pharmacy, pharmacology & toxicology
http://hdl.handle.net/2268/262193
Pegylated triarylmethanes: Synthesis, antimicrobial activity, anti-proliferative behavior and in silico studies
English
Ricco, Christophe [Conservatoire national des arts et métiers > Equipe de Chimie Moléculaire du Laboratoire Génomique, Bioinformatique et Chimie Moléculaire > > >]
Abdmouleh, Fatma [Conservatoire national des arts et métiers > > > >]
Riccobono, Charlotte [Conservatoire national des arts et métiers > > > >]
Guenineche, Lena [Conservatoire national des arts et métiers > > > >]
Martin, Frederique [Université de Limoges > > > >]
Goya-Jorge, Elizabeth mailto [Université de Liège - ULiège > Département de sciences des denrées alimentaires (DDA) > Gestion de la qualité dans la chaîne alimentaire >]
Liagre, Bertrand [Université de Limoges > > > >]
Ben Ali, Mamdouh [Université de Sfax > > > >]
Ferroud, Clotilde [Conservatoire national des arts et métiers > > > >]
EL Arbi, Mehdi [Université de Sfax > > > >]
Sylla-Iyarreta Veitía, Maité mailto [Conservatoire national des arts et métiers > Equipe de Chimie Moléculaire du Laboratoire Génomique, Bioinformatique et Chimie Moléculaire > > >]
22-Jan-2020
Bioorganic Chemistry
Elsevier
96
103591
Yes (verified by ORBi)
International
0045-2068
1090-2120
Atlanta
FL
[en] triarylmethane ; PEGylation ; antimicrobial activity ; anti-proliferative activity ; anti-biofilm activity ; drug-likeness
[en] We describe herein the synthesis, characterization and biological studies of novel PEGylated triarylmethanes. Non-symmetrical and symmetrical triarylmethanes series have been synthesized by Friedel-Crafts hydroxyalkylation or directly from bisacodyl respectively followed by a functionalization with PEG fragments in order to increase bioavailability and biological effectiveness. The antimicrobial activity was investigated against Gram-positive and Gram-negative foodborne pathogens and against Candida albicans, an opportunistic pathogenic yeast. The biocidal activity was also studied using Staphylococcus aureus as a reference bacterium. Almost all PEGylated molecules displayed an antifungal activity comparable with fusidic acid with MIC values ranging from 6.25 to 50 μg/mL. Compounds also revealed a promising anti-biofilm activity with biofilm eradication percentages values above 80% for the best molecules (compounds 4d and 7). Compounds 7 and 8b showed a modest antiproliferative activity against human colorectal cancer cell lines HT-29. Finally, in silico predictions suggested adequate ADME and drug-likeness profiles for the synthetized triarylmethanes.
Researchers
http://hdl.handle.net/2268/262193
10.1016/j.bioorg.2020.103591
https://www.sciencedirect.com/science/article/abs/pii/S0045206819320929

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