Details

Autor(en) / Beteiligte

• Cummings, Maxwell D
• Lin, Tse-I
• Hu, Lili
• Tahri, Abdellah
• McGowan, David
• Amssoms, Katie
• Last, Stefaan
• Devogelaere, Benoit
• Rouan, Marie-Claude
• Vijgen, Leen
• Berke, Jan Martin
• Dehertogh, Pascale
• Fransen, Els
• Cleiren, Erna
• vanderHelm, Liesbet
• Fanning, Gregory
• VanEmelen, Kristof
• Nyanguile, Origène
• Simmen, Kenny
• Raboisson, Pierre
• Vendeville, Sandrine

Titel

Structure-Based Macrocyclization Yields HepatitisC Virus NS5B Inhibitors with Improved Binding Affinities and Pharmacokinetic Properties

Ist Teil von

• Angewandte Chemie International Edition, 2012-05, Vol.51 (19), p.4637

Auflage

International ed. in English

Ort / Verlag

Weinheim: Wiley Subscription Services, Inc

Erscheinungsjahr

2012

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• The concept of drug-likeness distills the physicochemical properties of small-molecule drugs to a set of rules. Macrocyclic drugs are known to break these rules. A structure-based macrocyclization strategy was applied to design new hepatitisC virus NS5B inhibitors with improved pharmacokinetic properties, exemplifying a rational strategy for overcoming the confines of standard "drug-like chemical space".