title: Alternative core development around the tetracyclic indole class of HCV NS5A inhibitors.
abstract: Herein, we describe our research efforts to develop unique cores in molecules which function as HCV nonstructural protein 5A (NS5A) inhibitors. In particular, various fused tetracyclic cores were identified which showed genotype and mutant activities comparable to the indole-based tetracyclic core.
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Ling
authors.initials: L
authors.lastname: Tong
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Wensheng
authors.initials: W
authors.lastname: Yu
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Craig A
authors.initials: CA
authors.lastname: Coburn
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Peter T
authors.initials: PT
authors.lastname: Meinke
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Anilkumar G
authors.initials: AG
authors.lastname: Nair
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Michael P
authors.initials: MP
authors.lastname: Dwyer
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Lei
authors.initials: L
authors.lastname: Chen
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Oleg
authors.initials: O
authors.lastname: Selyutin
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Stuart B
authors.initials: SB
authors.lastname: Rosenblum
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Yueheng
authors.initials: Y
authors.lastname: Jiang
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: James
authors.initials: J
authors.lastname: Fells
authors.affiliation: Department of Medicinal Chemistry, WuXi AppTec, Shanghai 200131, China.
authors.forename: Bin
authors.initials: B
authors.lastname: Hu
authors.affiliation: Department of Medicinal Chemistry, WuXi AppTec, Shanghai 200131, China.
authors.forename: Bin
authors.initials: B
authors.lastname: Zhong
authors.affiliation: Department of Medicinal Chemistry, WuXi AppTec, Shanghai 200131, China.
authors.forename: Richard M
authors.initials: RM
authors.lastname: Soll
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Rong
authors.initials: R
authors.lastname: Liu
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Sony
authors.initials: S
authors.lastname: Agrawal
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Ellen
authors.initials: E
authors.lastname: Xia
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Ying
authors.initials: Y
authors.lastname: Zhai
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Rong
authors.initials: R
authors.lastname: Kong
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Paul
authors.initials: P
authors.lastname: Ingravallo
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Amin
authors.initials: A
authors.lastname: Nomeir
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Ernest
authors.initials: E
authors.lastname: Asante-Appiah
authors.affiliation: Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
authors.forename: Joseph A
authors.initials: JA
authors.lastname: Kozlowski
mesh_terms: D000998:Antiviral Agents / Q000494:pharmacology; D016174:Hepacivirus / Q000187:drug effects; D007211:Indoles / Q000494:pharmacology*; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors*; D012324:RNA-Dependent RNA Polymerase
chemical_list: D000998:Antiviral Agents; D007211:Indoles; D017361:Viral Nonstructural Proteins; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase
keywords: DAA; Direct-acting antiviral agents; Elbasvir; HCV NS5A inhibitor; HCV infection treatment; MK-8742; Tetracyclic core