Search

Your search keyword '"Frank Narjes"' showing total 4 results
Start Over Author "Frank Narjes" Search Limiters Peer Reviewed
4 results on '"Frank Narjes"'

2. Discovery of (7R)-14-Cyclohexyl-7-{[2-(dimethylamino)ethyl](methyl) amino}-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic Acid (MK-3281), a Potent and Orally Bioavailable Finger-Loop Inhibitor of the Hepatitis C Virus NS5B Polymerase.

Author

Frank Narjes, Benedetta Crescenzi, Marco Ferrara, Jörg Habermann, Stefania Colarusso, Maria del Rosario Rico Ferreira, Ian Stansfield, Angela Claire Mackay, Immacolata Conte, Caterina Ercolani, Simone Zaramella, Maria-Cecilia Palumbi, Philip Meuleman, Geert Leroux-Roels, Claudio Giuliano, Fabrizio Fiore, Stefania Di Marco, Paola Baiocco, Uwe Koch, and Giovanni Migliaccio

Subjects
*DRUG development, *CARBOXYLIC acids, *DRUG synergism, *HEPATITIS C virus, *VIRAL replication, *INDOLE, *MOLECULAR structure, *VIREMIA, *LABORATORY mice
Abstract

Infections caused by hepatitis C virus (HCV) are a significant world health problem for which novel therapies are in urgent demand. The polymerase of HCV is responsible for the replication of viral genome and has been a prime target for drug discovery efforts. Here, we report on the further development of tetracyclic indole inhibitors, binding to an allosteric site on the thumb domain. Structure−activity relationship (SAR) studies around an indolo-benzoxazocine scaffold led to the identification of compound 33(MK-3281), an inhibitor with good potency in the HCV subgenomic replication assay and attractive molecular properties suitable for a clinical candidate. The compound caused a consistent decrease in viremia in vivo using the chimeric mouse model of HCV infection. [ABSTRACT FROM AUTHOR]

Published
2011
Full Text
View/download PDF

4. Identification and Biological Evaluation of a Series of 1H-Benzo[de]isoquinoline-1,3(2H)-diones as Hepatitis C Virus NS5B Polymerase Inhibitors‡.

Author

Jesus M. Ontoria, Edwin H. Rydberg, Stefania Di Marco, Licia Tomei, Barbara Attenni, Savina Malancona, José I. Martin Hernando, Nadia Gennari, Uwe Koch, Frank Narjes, Michael Rowley, Vincenzo Summa, Steve S. Carroll, David B. Olsen, Raffaele De Francesco, Sergio Altamura, Giovanni Migliaccio, and Andrea Carfì

Published
2009
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results