title: Synthesis and evaluation of non-dimeric HCV NS5A inhibitors.
abstract: Based on the symmetrical bidentate structure of the NS5A inhibitor BMS-790052, a series of new monodentate molecules were designed. The synthesis of 36 new non-dimeric NS5A inhibitors is reported along with their ability to block HCV replication in an HCV 1b replicon system. Among them compound 5a showed picomolar range activity along with an excellent selectivity index (SI > 90,000).
authors: Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Veterans Affairs Medical Center, Decatur, GA 30033, USA.
authors: Franck
authors: F
authors: Amblard
authors: Hongwang
authors: H
authors: Zhang
authors: Longhu
authors: L
authors: Zhou
authors: Junxing
authors: J
authors: Shi
authors: Drew R
authors: DR
authors: Bobeck
authors: James H
authors: JH
authors: Nettles
authors: Satish
authors: S
authors: Chavre
authors: Tamara R
authors: TR
authors: McBrayer
authors: Philip
authors: P
authors: Tharnish
authors: Tony
authors: T
authors: Whitaker
authors: Steven J
authors: SJ
authors: Coats
authors: Raymond F
authors: RF
authors: Schinazi
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002219:Carbamates; D002460:Cell Line; D002522:Chlorocebus aethiops; D004305:Dose-Response Relationship, Drug; D016174:Hepacivirus / Q000187:drug effects; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011759:Pyrrolidines; D013329:Structure-Activity Relationship; D014633:Valine / Q000031:analogs & derivatives; D014709:Vero Cells; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors*; D014779:Virus Replication / Q000187:drug effects; D012324:RNA-Dependent RNA Polymerase
chemical_list: D000998:Antiviral Agents; D002219:Carbamates; D007093:Imidazoles; D011759:Pyrrolidines; D014633:Valine; D017361:Viral Nonstructural Proteins; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase; C549273:daclatasvir