Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Dominique Louis Nestor Ghislain Surleraux"'
Autor:
David Dukhan, Thierry Convard, Rachid Rahali, Agnès Amador, Anna Giulia Loi, Valeria Mascia, Massimiliano LaColla, Julien Milhau, Eric Badaroux, Maria Seifer, Loredana Onidi, Ludovic Griffe, Claire Pierra Rouviere, Joe McCarville, Dominique Louis Nestor Ghislain Surleraux, Efisio Sais, Daniel Da Costa, David Standring, Jean-François Griffon, Frédéric Leroy, Michel Liuzzi, Jean-Laurent Paparin, Cyril B. Dousson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:4536-4541
The hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) plays a central role in virus replication. NS5B has no functional equivalent in mammalian cells and, as a consequence, is an attractive target for selective inhibition. This Letter
Autor:
Thierry Convard, L.B. Lallos, Florence Bonnaterre, Valérie Bidau, Houcine Rahali, David Standring, Virginie Roques, Francois-Rene Alexandre, Maria Seifer, Anna-Giulia Loi, Damien Gloux, Christophe Claude Parsy, Elodie Rosinovsky, Dominique Chaves, Catherine Caillet, Frederic Leroy, Guillaume Brandt, Dominique Louis Nestor Ghislain Surleraux, Sylvie Cappelle, Yann Griffon, Simon Savin, Musiu Chiara, Laure Moulat, Michel Liuzzi, Michel Derock
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:5427-5436
Exploration of the P2 region by mimicking the proline motif found in BILN2061 resulted in the discovery of two series of potent HCV NS3/4A protease inhibitors. X-ray crystal structure of the ligand in contact with the NS3/4A protein and modulation of
Autor:
Jean-Pierre Sommadossi, Michel Liuzzi, Samira Benzaria-Prad, Anna Giulia Loi, Jerome Peyronnet, Claire Pierra, Dominique Louis Nestor Ghislain Surleraux, Gwenaëlle Sizun, Gilles Gosselin, Maria Seifer, Chiara Musiu, Eric Badaroux, Céline Rabeson, David Standring
Publikováno v:
Future Medicinal Chemistry. 7:1675-1700
Background: Ribonucleoside analogs possessing a β-methyl substituent at the 2′-position of the d-ribose moiety have been previously discovered to be potent and selective inhibitors of hepatitis C virus (HCV) replication, their triphosphates acting
Autor:
Yann Griffon, Michel Derock, Damien Gloux, Francois-Rene Alexandre, Maria Seifer, Chiara Musiu, Christophe Claude Parsy, Houcine Rahali, Dominique Louis Nestor Ghislain Surleraux, Anna-Giulia Loi, Sylvie Cappelle, Frederic Leroy, Thierry Convard, Guillaume Brandt, Dominique Chaves, L.B. Lallos, Virginie Roques, David Standring, Laure Moulat, Michel Liuzzi, Catherine Caillet
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:4444-4449
Structural homology between thrombin inhibitors and the early tetrapeptide HCV protease inhibitor led to the bioisosteric replacement of the P2 proline by a 2,4-disubstituted azetidine within the macrocyclic β-strand mimic. Molecular modeling guided
Autor:
Jean-Laurent Paparin, Thierry Convard, Catherine Caillet, Stéphanie Bot, Dominique Louis Nestor Ghislain Surleraux, Claire Pierra, Valeria Mascia, Maria Seifer, Jean-François Griffon, Efisio Sais, Agnès Amador, David Dukhan, Cyril B. Dousson, Elodie Rosinosky, Loredana Onidi, Anna Giulia Loi, Rachid Rahali, Eric Badaroux, Massimiliano LaColla, Frédéric Leroy, David Standring, Michel Liuzzi, Joe McCarville, Julien Milhau, Ludovic Griffe, Daniel Da Costa
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(11)
Hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) plays a central role in virus replication. NS5B has no functional equivalent in mammalian cells, and as a consequence is an attractive target for selective inhibition. This paper descri
Autor:
Michael Edlund, Oliver Lenz, Pia Cecilia Kahnberg, Stefan Lindström, Frederic Delouvroy, Dominique Louis Nestor Ghislain Surleraux, Magnus Nilsson, Dmitry Antonov, Anders Eneroth, Wim Van De Vreken, Kristina Wikström, Tse-I Lin, Piet Wigerinck, Kenneth Simmen, Vladimir Ivanov, Marleen Van Dooren, Susana Ayesa, Hu Lili, Abdellah Tahri, Åsa Rosenquist, Lotta Vrang, Per-Ola Johansson, Vendeville Sandrine Marie Hele, Herman de Kock, Pierre Raboisson, Bertil Samuelsson, Björn Classon, Natalie Maria Francisca Kindermans, David McGowan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:6189-6193
A novel series of P3-truncated macrocyclic HCV NS3/4A protease inhibitors containing a P2 proline-urea or carbamate scaffold was synthesized. Very potent inhibitors were obtained through the optimization of the macrocycle size, urea and proline subst
Autor:
Frederic Delouvroy, Dominique Louis Nestor Ghislain Surleraux, Herman de Kock, Oliver Lenz, David McGowan, Pierre Raboisson, Magnus Nilsson, Åsa Rosenquist, Wim Van De Vreken, Hu Lili, Piet Wigerinck, Tse-I Lin, Bertil Samuelsson, Abdellah Tahri, Vendeville Sandrine Marie Hele, Kenneth Simmen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5095-5100
Starting from the previously reported HCV NS3/4A protease inhibitor BILN 2061, we have used a fast-follower approach to identify a novel series of HCV NS3/4A protease inhibitors in which (i) the P3 amino moiety and its capping group have been truncat
Autor:
Dominique Louis Nestor Ghislain Surleraux, Erna Cleiren, Liesbet van der Helm, Origène Nyanguile, Pierre Raboisson, Wendy Mostmans, Ludo Maria Marcel Quirynen, Kenneth Simmen, Anne-Stéphanie Rueff, Carlo Boutton, Frederik Pauwels
Publikováno v:
Journal of Virology. 81:6909-6919
The search for hepatitis C virus polymerase inhibitors has resulted in the identification of several nonnucleoside binding pockets. The shape and nature of these binding sites differ across and even within diverse hepatitis C virus genotypes. These d
Autor:
Frederic Delouvroy, Katrien Vermeiren, Dominique Louis Nestor Ghislain Surleraux, Sarvajit Chakravarty, Annick Scholliers, Pierre Raboisson, Tse-I Lin, Thierry Verbinnen, Kenneth Simmen, Oliver Lenz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1843-1849
Screening of a focused library of TGF beta kinase inhibitors in the cellular HCV replicon model with luciferase read out yielded a number of low micromolar HCV inhibitors. Medicinal chemistry driven optimization resulted in the discovery of 4-[2-(5-b
Autor:
Dominique Louis Nestor Ghislain Surleraux, Yann Griffon, Christophe Claude Parsy, David Standring, Dominique Chaves, Houcine Rahali, Frederic Leroy, Chiara Musiu, Anna-Giulia Loi, L.B. Lallos, Catherine Caillet, Francois-Rene Alexandre, Maria Seifer, Michel Liuzzi, Damien Gloux, Laure Moulat, Thierry Convard, Michel Derock, Guillaume Brandt, Virginie Roques
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(18)
We disclose here the synthesis of a series of macrocyclic HCV protease inhibitors, where the homoserine linked together the quinoline P2' motif and the macrocyclic moiety. These compounds exhibit potent inhibitory activity against HCV NS3/4A protease