Inhibitors of hepatitis C virus NS3.4A protease 2. Warhead SAR and optimization.

Perni, Robert B; Pitlik, Janos; Britt, Shawn D; Court, John J; Courtney, Lawrence F; Deininger, David D; Farmer, Luc J; Gates, Cynthia A; Harbeson, Scott L; Levin, Rhonda B; Lin, Chao; Lin, Kai; Moon, Young-Choon; Luong, Yu-Ping; O'Malley, Ethan T; Rao, B Govinda; Thomson, John A; Tung, Roger D; Van Drie, John H; Wei, Yunyi

Perni, Robert B; Pitlik, Janos; Britt, Shawn D; Court, John J; Courtney, Lawrence F; Deininger, David D; Farmer, Luc J; Gates, Cynthia A; Harbeson, Scott L; Levin, Rhonda B; Lin, Chao; Lin, Kai; Moon, Young-Choon; Luong, Yu-Ping; O'Malley, Ethan T; Rao, B Govinda; Thomson, John A; Tung, Roger D; Van Drie, John H; Wei, Yunyi.

Affiliation

Perni RB; Vertex Pharmaceuticals Inc., 130 Waverly Street, Cambridge, MA 02139, USA.

Bioorg Med Chem Lett ; 14(6): 1441-6, 2004 Mar 22.

Article in En | MEDLINE | ID: mdl-15006379

ABSTRACT

The alpha-ketoamide warhead (e.g., 15) was found to be a practical replacement for aliphatic aldehydes in a series of HCV NS3.4A protease inhibitors. Structure-activity relationships and prime side optimization are discussed.

Subject(s)

Hepacivirus/enzymology; Macrocyclic Compounds; Quinolines; Serine Endopeptidases/metabolism; Serine Proteinase Inhibitors/chemistry; Viral Nonstructural Proteins/antagonists & inhibitors; Carbamates/chemistry; Carbamates/metabolism; Hepacivirus/drug effects; Structure-Activity Relationship; Thiazoles/chemistry; Thiazoles/metabolism; Viral Nonstructural Proteins/metabolism

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Collection: 01-internacional Database: MEDLINE Main subject: Quinolines / Serine Endopeptidases / Serine Proteinase Inhibitors / Viral Nonstructural Proteins / Hepacivirus / Macrocyclic Compounds Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2004 Type: Article Affiliation country: United States

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