Nie, Shenyou published the artcileSynthesis, Structure-Activity Relationships, and Antiviral Activity of Allosteric Inhibitors of Flavivirus NS2B-NS3 Protease, Application In Synthesis of 566205-01-4, the main research area is allosteric inhibitor flavivirus NS2B NS3 protease.
Flaviviruses, including Zika, dengue, and West Nile viruses, are important human pathogens. The highly conserved NS2B-NS3 protease of Flavivirus is essential for viral replication and therefore a promising drug target. Through compound screening, followed by medicinal chem. studies, a novel series of 2,5,6-trisubstituted pyrazine compounds are found to be potent, allosteric inhibitors of Zika virus protease (ZVpro) with IC50 values as low as 130 nM. Their structure-activity relationships are discussed. The ZVpro inhibitors also inhibit homologous proteases of dengue and West Nile viruses, and their inhibitory activities are correlated. The most potent compounds 47 and 103 potently inhibited Zika virus replication in cells with EC68 values of 300-600 nM and in a mouse model of Zika infection. These compounds represent novel pharmacol. leads for drug development against Flavivirus infections.
Journal of Medicinal Chemistry published new progress about Allosteric modulators. 566205-01-4 belongs to class pyrazines, name is 2-Amino-3,5-dibromo-6-chloropyrazine, and the molecular formula is C4H2Br2ClN3, Application In Synthesis of 566205-01-4.