1384259-02-2Relevant articles and documents
Structure-based macrocyclization yields hepatitis C virus NS5B inhibitors with improved binding affinities and pharmacokinetic properties
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,Van Der Helm, Liesbet,Fanning, Gregory,Van Emelen, Kristof,Nyanguile, Origene,Simmen, Kenny,Raboisson, Pierre,Vendeville, Sandrine
, p. 4637 - 4640 (2012)
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 hepatitis C virus NS5B inhibitors with improved pharmacokinetic properties, exemplifying a rational strategy for overcoming the confines of standard drug-like chemical space . Copyright