1108658-29-2Relevant articles and documents
Synthesis and antiviral evaluation of a novel series of homoserine-based inhibitors of the hepatitis C virus NS3/4A serine protease
Alexandre, Fran?ois-René,Brandt, Guillaume,Caillet, Catherine,Chaves, Dominique,Convard, Thierry,Derock, Michel,Gloux, Damien,Griffon, Yann,Lallos, Lisa,Leroy, Frédéric,Liuzzi, Michel,Loi, Anna-Giulia,Moulat, Laure,Musiu, Chiara,Parsy, Christophe,Rahali, Houcine,Roques, Virginie,Seifer, Maria,Standring, David,Surleraux, Dominique
, p. 3984 - 3991 (2015)
Abstract 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 and replicon cell based assay. Their enzymatic and antiviral activities are modulated by substitutions on the quinoline P2′ at position 8 by methyl and halogens and by small heterocycles at position 2. The in vitro structure activity relationship (SAR) studies and in vivo pharmacokinetic (PK) evaluations of selected compounds are described herein.
