Eric Bacqué
19 Papers
39 Citations
Eric Bacqué is an academic researcher. The author has contributed to research in topics: Chemistry & Moiety. The author has an hindex of 8, co-authored 11 publications.
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Papers
Thiophene antibacterials that allosterically stabilize DNA-cleavage complexes with DNA gyrase
Pan F. Chan,Thomas Germe,Benjamin D. Bax,Jianzhong Huang,Reema K. Thalji,Eric Bacqué,Anna Checchia,Dongzhao Chen,Haifeng Cui,Xiao Ding,Karen A. Ingraham,Lynn McCloskey,Kaushik Raha,Velupillai Srikannathasan,Anthony Maxwell,Robert A. Stavenger +15 more
TL;DR: A class of antibacterial thiophenes that target DNA gyrase with a unique mechanism of action and have activity against a range of bacterial pathogens, including strains resistant to fluoroquinolones are identified.
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A new class of antibacterials, the imidazopyrazinones, reveal structural transitions involved in DNA gyrase poisoning and mechanisms of resistance
Thomas Germe,Judit Vörös,Frédéric Jeannot,Thomas Taillier,Robert A. Stavenger,Eric Bacqué,Anthony Maxwell,Benjamin D. Bax,Benjamin D. Bax +8 more
TL;DR: The D82N mutant appears to act by stabilizing the binary conformation of DNA gyrase with uncleaved DNA without direct interaction with the compounds, which provides general insight into the resistance mechanisms to antibiotics targeting bacterial type II topoisomerases.
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Discovery and Pharmacokinetic and Pharmacological Properties of the Potent and Selective MET Kinase Inhibitor 1-{6-[6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanyl]benzothiazol-2-yl}-3-(2-morpholin-4-ylethyl)urea (SAR125844).
Antonio Ugolini,Mireille Kenigsberg,Alexey Rak,François Vallée,Jacques Houtmann,Maryse Lowinski,Cécile Capdevila,Jean Khider,Eva Albert,Nathalie Martinet,Conception Nemecek,Sandrine Grapinet,Eric Bacqué,Manfred Roesner,Christine Delaisi,Loreley Calvet,Fabrice Bonche,Dorothée Semiond,Coumaran Egile,Hélène Goulaouic,Laurent Schio +20 more
TL;DR: A series of triazolopyridazines that are selective inhibitors of wild-type (WT) MET kinase and several clinically relevant mutants are discovered and insight is provided into their mode of binding and unprecedented crystal structures of the Y1230H variant are reported.
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Identification and optimization of a new series of anti-tubercular quinazolinones.
Cédric Couturier,Christine Lair,Alain Pellet,Anna M. Upton,Takushi Kaneko,Corinne Perron,Eric Cogo,Jerome Menegotto,Armin Bauer,Bodo Scheiper,Sophie Lagrange,Eric Bacqué +11 more
TL;DR: A high throughput phenotypic screening against Mycobacterium smegmatis led to the discovery of a new class of bacteriostatic, highly hydrophobic antitubercular quinazolinones that potently inhibited the in vitro growth of either extracellular or intramacrophagic M. tuberculosis (Mtb), via modulation of an unidentified but yet novel target.
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