Discovery of ravidasvir (PPI-668) as a potent pan-genotypic HCV NS5A inhibitor

Nonconjugated Hydrocarbons as Rigid‐Linear Motifs: Isosteres for Material Sciences and Bioorganic and Medicinal Chemistry

“…Alternative rigid bioisosteres, such as the BCO analogue 337,w ere employed to improvet he pharmacokinetic properties of the compound. [433] Resultss howed good solubility and potency at the target. Additionally, the BCO derivative 337 possessedg ood bioavailability and highc oncentrations in liver tissues and saw increased solubility compared with the parentc ompound.…”

Twelve‐week ravidasvir plus ritonavir‐boosted danoprevir and ribavirin for non‐cirrhotic HCV genotype 1 patients: A phase 2 study

“…Ravidasvir (RDV, ASC16) is a second‐generation, pan‐genotypic non‐structural (NS) 5A inhibitor, which inhibits viral replication and assembly . RDV exhibits high antiviral potency with EC 50 0.04–1.14 nM for HCV GT1–GT6.…”

“…4 Ravidasvir (RDV, ASC16) is a second-generation, pangenotypic non-structural (NS) 5A inhibitor, which inhibits viral replication and assembly. 5,6 RDV exhibits high antiviral potency with EC 50 0.04-1.14 nM for HCV GT1-GT6. The pharmacokinetics results indicated that steady status achieved quickly after the first dose.…”

Palladium-Catalyzed C–H Heteroarylation of 2,5-Disubstituted Imidazoles

“…More generally, arylated imidazoles are a fundamental scaffold of various drug-lead molecules. [12][13][14][15][16][17][18][19][20] The synthesis of N-heteroarylated imidazoles via C-H activation, however, has not been systematically studied.…”