Discovery and structural diversity of the hepatitis C virus NS3/4A serine protease inhibitor series leading to clinical candidate IDX320

[Display omitted] 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 the quinoline heterocyclic regi...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2015-11, Vol.25 (22), p.5427-5436
Hauptverfasser:	Parsy, Christophe C., Alexandre, François-René, Bidau, Valérie, Bonnaterre, Florence, Brandt, Guillaume, Caillet, Catherine, Cappelle, Sylvie, Chaves, Dominique, Convard, Thierry, Derock, Michel, Gloux, Damien, Griffon, Yann, Lallos, Lisa B., Leroy, Frederic, Liuzzi, Michel, Loi, Anna-Giulia, Moulat, Laure, Chiara, Musiu, Rahali, Houcine, Roques, Virginie, Rosinovsky, Elodie, Savin, Simon, Seifer, Maria, Standring, David, Surleraux, Dominique
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Drug Discovery Haplorhini HCV NS3/4A protease inhibitors Hepacivirus - drug effects Hepatitis C Hepatocytes - enzymology Humans Inhibitory Concentration 50 Macrocycle Macrocyclic Compounds - chemistry Macrocyclic Compounds - pharmacology Mice Microsomes, Liver - enzymology Molecular Structure Rats Rats, Sprague-Dawley Serine Proteinase Inhibitors - chemical synthesis Serine Proteinase Inhibitors - chemistry Serine Proteinase Inhibitors - pharmacology Viral Nonstructural Proteins - antagonists & inhibitors Viral Nonstructural Proteins - chemistry
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