367259-52-7Relevant articles and documents
Potent 7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid-based macrocyclic inhibitors of hepatitis C virus NS3 protease
Chen, Kevin X.,Njoroge, F. George,Pichardo, John,Prongay, Andrew,Butkiewicz, Nancy,Yao, Nanhua,Madison, Vincent,Girijavallabhan, Viyyoor
, p. 567 - 574 (2007/10/03)
The NS3 protease of hepatitis C virus (HCV) has emerged as one of the best characterized targets for next-generation HCV therapy. The tetrapeptide 1 and pentapeptide 2 are α-ketoamide-type HCV serine protease inhibitors with modest potency. We envisioned
Design, synthesis, and biological activity of m-tyrosine-based 16- and 17-membered macrocyclic inhibitors of hepatitis C virus NS3 serine protease
Chen, Kevin X.,Njoroge, F. George,Pichardo, John,Prongay, Andrew,Butkiewicz, Nancy,Yao, Nanhua,Madison, Vincent,Girijavallabhan, Viyyoor
, p. 6229 - 6235 (2007/10/03)
The limited efficacy and considerable side effects of currently available therapies for the treatment of hepatitis C virus (HCV) infection have prompted significant efforts toward the development of safe and effective new therapeutics. The pentapeptide α-
Proline-based macrocyclic inhibitors of the hepatitis C virus: Stereoselective synthesis and biological activity
Chen, Kevin X.,Njoroge, F. George,Vibulbhan, Bancha,Prongay, Andrew,Pichardo, John,Madison, Vincent,Buevich, Alexei,Chan, Tze-Ming
, p. 7024 - 7028 (2007/10/03)
Life-saving donut: Macrocyclization through a Mitsunobu reaction was used to synthesize a 17-membered macrocycle. The bicyclic acetal core was prepared completely diastereoselectively. The macrocyclic peptidomimetic surrogate of the P2-P3 dipeptide moiety was designed to function as a hepatitis C virus (HCV) NS3 serine protease inhibitor, and the pentapeptide α-ketoamides derived from the macrocycle were shown to be potent HCV inhibitors. (Figure Presented).