Bogen Stéphane L, Ruan Sumei, Liu Rong, Agrawal Sony, Pichardo John, Prongay Andrew, Baroudy Bahige, Saksena Anil K, Girijavallabhan Viyyoor, Njoroge F George
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Bioorg Med Chem Lett. 2006 Mar 15;16(6):1621-7. doi: 10.1016/j.bmcl.2005.12.013. Epub 2006 Jan 4.
Depeptidization efforts of the P(3)-P(2) region of P(3) capped alpha-ketoamide inhibitor of HCV NS3 serine protease 1 are reported. We clearly established that N-methylation of the P(2) nitrogen and modification of the P(2)' carboxylic acid terminus were essential for activity in the replicon assay.
报道了对丙型肝炎病毒NS3丝氨酸蛋白酶1的P(3)封端的α-酮酰胺抑制剂的P(3)-P(2)区域进行去肽化的研究。我们明确证实，P(2)氮原子的N-甲基化和P(2)'羧酸末端的修饰对于复制子试验中的活性至关重要。
