Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Vincent Gerusz"'
Publikováno v:
Synthesis. 49:5320-5334
A series of 1,5-anhydro- d - glycero - d - gluco -heptitol derivatives have been prepared from 3- O -benzyl-1,2- O -isopropylidene- d - glycero - d - gluco -heptofuranose via conversion into anomeric bromide and thiophenyl derivatives, followed by gl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8ae785713044b6b5e2dbf4e2e33a0d04
https://doi.org/10.1055/s-0036-1591518
https://doi.org/10.1055/s-0036-1591518
Autor:
Mayalen Oxoby, François Moreau, Elodie Drocourt, Dmytro Atamanyuk, Benoit Ledoussal, Vincent Gerusz, Fabien Faivre
Publikováno v:
Journal of Medicinal Chemistry. 56:1908-1921
In this paper, we present different strategies to vectorize HldE kinase inhibitors with the goal to improve their gram-negative intracellular concentration. Syntheses and biological effects of siderophoric, aminoglycosidic, amphoteric, and polycation
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c0bb30726e6c11eeafb71465e3a9f57b
https://doi.org/10.1021/jm400097h
https://doi.org/10.1021/jm400097h
Autor:
Cédric Raymond, François Moreau, Laure Prouvensier, Jean-Marie Genevard, Yannick Bonvin, Lionel Durant, Laëtitia Peltier, Armelle Walton, Coralie Soulama-Mouze, Stéphanie Floquet, Elodie Drocourt, Vincent Gerusz, Mayalen Oxoby, Sonia Escaich, Géraldine LeFralliec, Vanessa Sam-Sambo, Vanida Vongsouthi, Nicolas Desroy, Marc Saccomani, Chrystelle Oliveira, Sophia Briet, Alexis Denis, Fabien Faivre
Publikováno v:
Journal of Medicinal Chemistry. 55:9914-9928
In this paper, we present some elements of our optimization program to decouple triclosan's specific FabI effect from its nonspecific cytotoxic component. The implementation of this strategy delivered highly specific, potent, and nonbiocidal new FabI
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b8cec45f475491713180acfabe1b6f5a
https://doi.org/10.1021/jm301113w
https://doi.org/10.1021/jm301113w
Autor:
Kirsty Maher, M. Saccomani, Vincent Gerusz, L. Prouvensier, Ian Morrissey, Vanida Vongsouthi, Sonia Escaich, C. Soulama-Mouze, L. Durant, M. Oxoby, François Moreau
Publikováno v:
Antimicrobial Agents and Chemotherapy. 55:4692-4697
MUT056399 is a highly potent new inhibitor of the FabI enzyme of both Staphylococcus aureus and Escherichia coli. In vitro , MUT056399 was very active against S. aureus strains, including methicillin-susceptible S. aureus (MSSA), methicillin-resistan
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc03a8e115aafa5fca2f040a5301f25a
https://doi.org/10.1128/aac.01248-10
https://doi.org/10.1128/aac.01248-10
Autor:
Stéphanie Floquet, Maxime Durka, Stéphane P. Vincent, Mounir Andaloussi, Régis Périon, Elodie Malacain, Vincent Gerusz, Michael Bosco, Mayalen Oxoby, Abdellatif Tikad, François Moreau
Publikováno v:
Chemistry - A European Journal. 17:11305-11313
L-Heptoses (L-glycero-D-manno-heptopyranoses) are constituents of the inner core of lipolysaccharide (LPS), a molecule playing key roles in the mortality of many infectious diseases as well as in the virulence of many human pathogens. The inhibition
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a6219ee91243f8ae9b5eae543828333
https://doi.org/10.1002/chem.201100396
https://doi.org/10.1002/chem.201100396
Autor:
Lionel Durant, Sonia Escaich, Jean-Marie Genevard, Alexis Denis, François Moreau, Mayalen Oxoby, Vincent Gerusz, Vanida Vongsouthi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3486-3490
Haspin is a serine/threonine kinase required for completion of normal mitosis that is highly expressed during cell proliferation, including in a number of neoplasms. Consequently, it has emerged as a potential therapeutic target in oncology. A high t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8fb23333c6fec52e747e2cf542177e92
https://doi.org/10.1016/j.bmcl.2010.05.004
https://doi.org/10.1016/j.bmcl.2010.05.004
Autor:
Alexis Denis, Nicolas Desroy, Sonia Escaich, Lionel Durant, Vincent Gerusz, Vanida Vongsouthi, Géraldine Le Fralliec, François Moreau, Stéphanie Floquet, Sophia Briet
Publikováno v:
Bioorganic & Medicinal Chemistry. 17:1276-1289
Gram-negative bacteria lacking heptoses in their lipopolysaccharide (LPS) display attenuated virulence and increased sensitivity to human serum and to some antibiotics. Thus inhibition of bacterial heptose synthesis represents an attractive target fo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5c8e0751613ede387a95852db1e194a
https://doi.org/10.1016/j.bmc.2008.12.021
https://doi.org/10.1016/j.bmc.2008.12.021
Autor:
Nicolas Desroy, Vanida Vongsouthi, Stéphanie Floquet, Dmytro Atamanyuk, Vincent Gerusz, Géraldine LeFralliec, François Moreau, Theodore B. Verhey, Ting-Wai Lee, Lionel Durant, Yannick Bonvin, Sophia Briet, Alexis Denis, Mayalen Oxoby, Fabien Faivre, Elodie Drocourt, Sonia Escaich, Chrystelle Oliveira, Murray S. Junop
Publikováno v:
Journal of medicinal chemistry. 56(4)
We report here the optimization of an HldE kinase inhibitor to low nanomolar potency, which resulted in the identification of the first reported compounds active on selected E. coli strains. One of the most interesting candidates, compound 86, was sh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2890016c6843ce1a2e7be486ac05f257
https://pubmed.ncbi.nlm.nih.gov/23409840
https://pubmed.ncbi.nlm.nih.gov/23409840
Autor:
Vincent Gerusz
Publisher Summary The bacterial fatty acid biosynthesis pathway has recently generated much interest for the development of novel classes of antibacterial agents. The organization of the bacterial fatty acid synthase type II system (FASII system) bas
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::52ae3874a21e93b4633a2b831c650bb3
https://doi.org/10.1016/s0065-7743(10)45018-6
https://doi.org/10.1016/s0065-7743(10)45018-6
Autor:
Jean-Marie Genevard, Vanida Vongsouthi, M. Busemann, K. Wolf, G. Le Fralliec, A. Aschenbrenner, Alexis Denis, Vincent Gerusz, Chrystelle Oliveira, Sonia Escaich, Nicolas Desroy, Stéphanie Floquet, François Moreau
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(14)
Heptosyltransferases such as WaaC represent promising and attractive targets for the discovery of new Gram-negative antibacterial drugs based on antivirulence mechanisms. We report herein our approach to the identification of the first micromolar inh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0f2874b0abf51160955764f15f402dc
https://pubmed.ncbi.nlm.nih.gov/18571407
https://pubmed.ncbi.nlm.nih.gov/18571407