Bennett, Frank; Kezar, Hollis S.; Girijavallabhan, Vinay; Huang, Yuhua; Huelgas, Regina; Rossman, Randall; Shih, Neng-Yang; Piwinski, John J.; MacCoss, Malcolm; Kwong, Cecil D.; Clark, Jeremy L.; Fowler, Anita T.; Geng, Feng; Roychowdhury, Abhijit; Reynolds, Robert C.; Maddry, Joseph A.; Ananthan, Subramaniam; Secrist, John A.; Li, Cheng; Chase, Robert; Curry, Stephanie; Huang, Hsueh-Cheng; Tong, Xiao; George Njoroge, F.; Arasappan, Ashok published the artcile< Pyridofuran substituted pyrimidine derivatives as HCV replication (replicase) inhibitors>, Application In Synthesis of 188057-20-7, the main research area is regioselective alkylation carbocyclic nucleoside preparation antiviral structure activity; pyridofuran pyrimidine nucleoside preparation antiviral replicase inhibitor HCV benzofuran.
Introduction of nitrogen atom into the benzene ring of a previously identified HCV replication (replicase) benzofuran inhibitor I (X = CH), resulted in the discovery of the more potent pyridofuran analog I (X = N). Subsequent introduction of small alkyl and alkoxy ligands into the pyridine ring resulted in further improvements in replicon potency. Replacement of the 4-chloro moiety on the pyrimidine core with a Me group, and concomitant mono-alkylation of the C-2 amino moiety resulted in the identification of several inhibitors with desirable characteristics. Nucleoside inhibitor II (R = CF3, R1 = Et, R2 = H; R = cyclopropyl, R1 = OEt, R2 = Me), from the mono-substituted pyridofuran and inhibitor 50 from the disubstituted series displayed excellent potency, selectivity (GAPDH/MTS CC50) and PK parameters in all species studied, while the selectivity in the thymidine incorporation assay (DNA·CC50) was low.
Bioorganic & Medicinal Chemistry Letters published new progress about Antiviral agents. 188057-20-7 belongs to class iodides-buliding-blocks, and the molecular formula is C5H4INO, Application In Synthesis of 188057-20-7.
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com