mk-7009 and succinamide

mk-7009 has been researched along with succinamide* in 1 studies

Other Studies

1 other study(ies) available for mk-7009 and succinamide

Article	Year
Novel P2-P4 macrocyclic inhibitors of HCV NS3/4A protease by P3 succinamide fragment depeptidization strategy. Bioorganic & medicinal chemistry letters, 2010, Jan-01, Volume: 20, Issue:1 Hepatitis C represents a serious worldwide health-care problem. Recently, we have disclosed a novel class of P2-P4 macrocyclic inhibitors of NS3/4A protease containing a carbamate functionality as capping group at the P3 N-terminus. Herein we report our work aimed at further depeptidizing the P3 region by replacement of the urethane function with a succinamide motif. This peptidomimetic approach has led to the discovery of novel P2-P4 macrocyclic inhibitors of HCV NS3/4A protease with sub-nanomolar enzyme affinities. In addition to being potent inhibitors of HCV subgenomic replication, optimized analogues within this series have also presented attractive PK properties and showed promising liver levels in rat following oral administration. Topics: Administration, Oral; Amides; Animals; Antiviral Agents; Binding Sites; Cell Line; Computer Simulation; Cyclopropanes; Humans; Indoles; Isoindoles; Lactams, Macrocyclic; Leucine; Proline; Protease Inhibitors; Rats; Rats, Wistar; Succinates; Sulfonamides; Viral Nonstructural Proteins	2010

Article

Year

Novel P2-P4 macrocyclic inhibitors of HCV NS3/4A protease by P3 succinamide fragment depeptidization strategy.

Bioorganic & medicinal chemistry letters, 2010, Jan-01, Volume: 20, Issue:1

Hepatitis C represents a serious worldwide health-care problem. Recently, we have disclosed a novel class of P2-P4 macrocyclic inhibitors of NS3/4A protease containing a carbamate functionality as capping group at the P3 N-terminus. Herein we report our work aimed at further depeptidizing the P3 region by replacement of the urethane function with a succinamide motif. This peptidomimetic approach has led to the discovery of novel P2-P4 macrocyclic inhibitors of HCV NS3/4A protease with sub-nanomolar enzyme affinities. In addition to being potent inhibitors of HCV subgenomic replication, optimized analogues within this series have also presented attractive PK properties and showed promising liver levels in rat following oral administration.

Topics: Administration, Oral; Amides; Animals; Antiviral Agents; Binding Sites; Cell Line; Computer Simulation; Cyclopropanes; Humans; Indoles; Isoindoles; Lactams, Macrocyclic; Leucine; Proline; Protease Inhibitors; Rats; Rats, Wistar; Succinates; Sulfonamides; Viral Nonstructural Proteins

2010