| Autor: |
L. Bogen, Stéphane, Arasappan, Ashok, Bennett, Frank, Chen, Kevin, Jao, Edwin, Liu, Yi-Tsung, G. Lovey, Raymond, Venkatraman, Srikanth, Pan, Weidong, Parekh, Tajel, E. Pike, Russel, Ruan, Sumei, Liu, Rong, Baroudy, Bahige, Agrawal, Sony, Chase, Robert, Ingravallo, Paul, Pichardo, John, Prongay, Andrew, Brisson, Jean-Marc, Y. Hsieh, Tony, Cheng, Kuo-Chi, J. Kemp, Scott, E. Levy, Odile, Lim-Wilby, Marguerita, Y. Tamura, Susan, K. Saksena, Anil, Girijavallabhan, Viyyoor, George Njoroge, F. |
| Zdroj: |
Journal of Medicinal Chemistry; May 2006, Vol. 49 Issue: 9 p2750-2757, 8p |
| Abstrakt: |
Introduction of various modified prolines at P2 and optimization of the P1 side chain led to the discovery of SCH6 (24, Table 2), a potent ketoamide inhibitor of the HCV NS3 serine protease. In addition to excellent enzyme potency (Ki*= 3.8 nM), 24 was also found to be a potent inhibitor of HCV subgenomic RNA replication with IC50 and IC90 of 40 and 100 nM, respectively. Recently, antiviral activity of 24 was demonstrated with inhibition of the full-length genotype 2a HCV genome. In addition, 24 was found to restore the responsiveness of the interferon regulatory factor 3 (IRF-3) in cells containing HCV RNA replicons. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
|
