Synthesis and biological activity of macrocyclic inhibitors of hepatitis C virus (HCV) NS3 protease.
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Chen KX, Njoroge FG, Prongay A, Pichardo J, Madison V, Girijavallabhan V
Synthesis and biological activity of macrocyclic inhibitors of hepatitis C virus (HCV) NS3 protease.
Bioorg Med Chem Lett. 2005 Oct 15;15(20):4475-8.
- PubMed ID
- 16112859 [ View in PubMed]
- Abstract
The 17-membered phenylalanine-based macrocycle 6 was prepared starting from 3-iodo-phenylalanine. Macrocyclization of alkene phenyl iodide 5 was effected through a palladium-catalyzed Heck reaction. The macrocyclic alpha-ketoamides were active inhibitors of the HCV NS3 protease, with the C-terminal acids and amides being more potent than tert-butyl esters.