945255-52-7Relevant articles and documents
Inhibitors of hepatitis C virus NS3·4A protease. Effect of P4 capping groups on inhibitory potency and pharmacokinetics
Perni, Robert B.,Chandorkar, Gurudatt,Cottrell, Kevin M.,Gates, Cynthia A.,Lin, Chao,Lin, Kai,Luong, Yu-Ping,Maxwell, John P.,Murcko, Mark A.,Pitlik, Janos,Rao, Govinda,Schairer, Wayne C.,Drie, John Van,Wei, Yunyi
, p. 3406 - 3411 (2008/02/08)
Reversible tetrapeptide-based compounds have been shown to effectively inhibit the hepatitis C virus NS3·4A protease. Inhibition of viral replicon RNA production in Huh-7 cells has also been demonstrated. We show herein that the inclusion of hydrogen bond donors on the P4 capping group of tetrapeptide-based inhibitors result in increased binding potency to the NS3·4A protease. The capping groups also impart significant effects on the pharmacokinetic profile of these inhibitors.
