tolcapone has been researched along with benzamide* in 1 studies
1 other study(ies) available for tolcapone and benzamide
| Article | Year |
|---|---|
Beyond Basicity: Discovery of Nonbasic DENV-2 Protease Inhibitors with Potent Activity in Cell Culture.
The viral serine protease NS2B-NS3 is one of the promising targets for drug discovery against dengue virus and other flaviviruses. The molecular recognition preferences of the protease favor basic, positively charged moieties as substrates and inhibitors, which leads to pharmacokinetic liabilities and off-target interactions with host proteases such as thrombin. We here present the results of efforts that were aimed specifically at the discovery and development of noncharged, small-molecular inhibitors of the flaviviral proteases. A key factor in the discovery of these compounds was a cellular reporter gene assay for the dengue protease, the DENV2proHeLa system. Extensive structure-activity relationship explorations resulted in novel benzamide derivatives with submicromolar activities in viral replication assays (EC Topics: Animals; Benzamides; Cell Survival; Dengue Virus; Drug Stability; Genes, Reporter; HeLa Cells; Humans; Microsomes, Liver; Protease Inhibitors; Rats; Small Molecule Libraries; Structure-Activity Relationship; Viral Nonstructural Proteins; Virus Replication | 2021 |