Výsledky vyhledávání - "Jean-Philippe Surivet"

Discovery of Novel Inhibitors of LpxC Displaying Potent in Vitro Activity against Gram-Negative Bacteria

Publikováno v: Journal of Medicinal Chemistry. 63:66-87

UDP-3-O-((R)-3-hydroxymyristoyl)-N-glucosamine deacetylase (LpxC) is as an attractive target for the discovery and development of novel antibacterial drugs to address the critical medical need created by multidrug resistant Gram-negative bacteria. By

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https://doi.org/10.1021/acs.jmedchem.9b01604

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Optimization of LpxC Inhibitor Lead Compounds Focusing on Efficacy and Formulation for High Dose Intravenous Administration

Autor: Michel Enderlin-Paput, Swen Seeland, A.-C. Blumstein, Daniel Ritz, Peter Seiler, R. Lange, Jean-Philippe Surivet, Christine Schmitt, F. Masse, Jean-Christophe Gauvin, S. Diethelm, L. Jacob, Charlyse Herrmann, Carmela Gnerre, Hans H. Locher, G. Mathieu, Azely Mirre, Georg Rueedi, Philippe Panchaud

Publikováno v: Journal of medicinal chemistry. 63(1)

LpxC inhibitors were optimized starting from lead compounds with limited efficacy and solubility and with the goal to provide new options for the treatment of serious infections caused by Gram-negative pathogens in hospital settings. To enable the de

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https://pubmed.ncbi.nlm.nih.gov/31804829

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Synthesis and Characterization of Tetrahydropyran-Based Bacterial Topoisomerase Inhibitors with Antibacterial Activity against Gram-Negative Bacteria

Autor: Thierry Bruyère, Eric A. Ertel, Stephanie Enderlin-Paput, Hans H. Locher, Michel Enderlin-Paput, Daniel Ritz, Christopher Kohl, Jean-Christophe Gauvin, Patrick Hess, Jean-Philippe Surivet, Azely Mirre, Daniel Bur, Cornelia Zumbrunn, Georg Rueedi, Christian Hubschwerlen, Peter Seiler

Publikováno v: Journal of Medicinal Chemistry. 60:3776-3794

There is an urgent unmet medical need for novel antibiotics that are effective against a broad range of bacterial species, especially multidrug resistant ones. Tetrahydropyran-based inhibitors of bacterial type II topoisomerases (DNA gyrase and topoi

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https://doi.org/10.1021/acs.jmedchem.6b01831

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In Vivo Pharmacodynamic Target Investigation of Two Bacterial Topoisomerase Inhibitors, ACT-387042 and ACT-292706, in the Neutropenic Murine Thigh Model against Streptococcus pneumoniae and Staphylococcus aureus

Autor: Daniel Ritz, David R. Andes, Jean-Philippe Surivet, Christopher Kohl, Alex Lepak, Peter Seiler

Publikováno v: Antimicrobial Agents and Chemotherapy. 60:3626-3632

ACT-387042 and ACT-292706 are two novel bacterial topoisomerase inhibitors with broad-spectrum activity against Gram-positive and -negative bacteria, including methicillin-resistant Staphylococcus aureus and penicillin- and fluoroquinolone-resistant

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https://doi.org/10.1128/aac.00363-16

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Design, Synthesis, and Characterization of Novel Tetrahydropyran-Based Bacterial Topoisomerase Inhibitors with Potent Anti-Gram-Positive Activity

Autor: Daniel Bur, Azely Mirre, Michel Enderlin-Paput, Georg Rueedi, Christian Hubschwerlen, Hans H. Locher, Daniel Ritz, Cornelia Zumbrunn, Wolfgang Keck, Maria Boehme, Marina Dos Santos, Jean-Christophe Gauvin, Peter Seiler, Jean-Philippe Surivet, Verena Kaegi, Jonathan Delers, Christopher Kohl, Thierry Bruyère, Mika Gaertner

Publikováno v: Journal of Medicinal Chemistry. 56:7396-7415

There is an urgent need for new antibacterial drugs that are effective against infections caused by multidrug-resistant pathogens. Novel nonfluoroquinolone inhibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) have the pote

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https://doi.org/10.1021/jm400963y

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An Atom-Economic Three-Carbon Chain Extension to Give Enamides

Autor: Jean-Philippe Surivet, Barry M. Trost

Publikováno v: Angewandte Chemie International Edition. 40:1468-1471

Di- or trisubstituted alkenes of defined geometry, with terminal enamide groups, are formed in an atom-economic three-carbon chain extension of alkynes with allyl amides catalyzed by ruthenium (see, for example, Equation (1); Boc=tert-butoxycarbonyl,

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https://doi.org/10.1002/1521-3773(20010417)40:8<1468::aid-anie1468>3.0.co

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Total synthesis of antitumor Goniothalamus styryllactones

Autor: Jean-Philippe Surivet, Jean-Michel Vatèle

Publikováno v: Tetrahedron. 55:13011-13028

Synthesis of eight enantiopure styryllactones has been achieved from a common precursor: ethyl (2S, 3S, 4R)-4-(t-butyldimethylsilyloxy)-2,3-isopropylidenedioxy-4-phenylbutanoate16, prepared in five steps and 65 % yield from (R)-mandelic acid. Key ele

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https://doi.org/10.1016/s0040-4020(99)00794-2

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Concise total synthesis of (+)-goniofufurone and goniobutenolides A and B

Autor: Jean-Michel Vatèle, Jean-Philippe Surivet

Publikováno v: Tetrahedron Letters. 37:4373-4376

Cytotoxic styryl lactones, (+)-goniofufurone and goniobutenolides A and B have been prepared in optically and diastereomerically pure form from (R)-(−)-mandelic acid via the β-hydroxy sulfone 4 as a common intermediate.

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https://doi.org/10.1016/0040-4039(96)00820-9

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