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Frank Narjes

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Frank Narjes; Maria-Cecilia Palumbi; Ian Stansfield; Simone Zaramella; Sergio Altamura; Paola Baiocco; Stefania Colarusso; Immacolata Conte; Benedetta Crescenzi; Raffaele De Francesco; Stefania Di Marco; Caterina Ercolani; Marco Ferrara; Maria del Rosario Rico Ferreira; Fabrizio Fiore; Claudio Giuliano; Jörg Habermann; Uwe Koch; Ralph Laufer; Geert Leroux-Roels; Angela Claire Mackay; Philip Meuleman; Giovanni Migliaccio; Michael Rowley
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.
Simona Cianetti; Vincent Brett Cooper; Barbara Attenni; Vincenzo Pucci; Fabrizio Fiore; Claudio Giuliano; Ralph Laufer; Cristina Gardelli; Edith Monteagudo; Frank Narjes; Gareth Edward Pearce; Michael Rowley
Enhancement of intestinal absorption of 2-methyl cytidine prodrugs.
Megan H Powdrill; Jerome Deval; Frank Narjes; Raffaele De Francesco; Matthias Götte
Mechanism of hepatitis C virus RNA polymerase inhibition with dihydroxypyrimidines.

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All Publications

2011: Frank Narjes; Maria-Cecilia Palumbi; Ian Stansfield; Simone Zaramella; Sergio Altamura; Paola Baiocco; Stefania Colarusso; Immacolata Conte; Benedetta Crescenzi; Raffaele De Francesco; Stefania Di Marco; Caterina Ercolani; Marco Ferrara; Maria del Rosario Rico Ferreira; Fabrizio Fiore; Claudio Giuliano; Jörg Habermann; Uwe Koch; Ralph Laufer; Geert Leroux-Roels; Angela Claire Mackay; Philip Meuleman; Giovanni Migliaccio; Michael Rowley
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.
Journal of medicinal chemistry 2011;54(1):289-301.
2010: Simona Cianetti; Vincent Brett Cooper; Barbara Attenni; Vincenzo Pucci; Fabrizio Fiore; Claudio Giuliano; Ralph Laufer; Cristina Gardelli; Edith Monteagudo; Frank Narjes; Gareth Edward Pearce; Michael Rowley
Enhancement of intestinal absorption of 2-methyl cytidine prodrugs.
Drug delivery 2010;17(4):214-22.
2010: Megan H Powdrill; Jerome Deval; Frank Narjes; Raffaele De Francesco; Matthias Götte
Mechanism of hepatitis C virus RNA polymerase inhibition with dihydroxypyrimidines.
Antimicrobial agents and chemotherapy 2010;54(3):977-83.
2009: Barbara Pacini; Salvatore Avolio; Caterina Ercolani; Uwe Koch; Giovanni Migliaccio; Frank Narjes; Laura Pacini; Licia Tomei; Steven Harper
2-(3-Thienyl)-5,6-dihydroxypyrimidine-4-carboxylic acids as inhibitors of HCV NS5B RdRp.
Bioorganic & medicinal chemistry letters 2009;19(21):6245-9.
2009: Jose Ignacio Martin Hernando; Jesus Maria Ontoria; Savina Malancona; Barbara Attenni; Fabrizio Fiore; Fabio Bonelli; Uwe Koch; Stefania Di Marco; Stefania Colarusso; Simona Ponzi; Nadia Gennari; Sue Ellen Vignetti; Maria Del Rosario Rico Ferreira; Jörg Habermann; Michael Rowley; Frank Narjes
Optimization of thienopyrrole-based finger-loop inhibitors of the hepatitis C virus NS5B polymerase.
ChemMedChem 2009;4(10):1695-713.
2009: Cristina Gardelli; Barbara Attenni; Monica Donghi; Malte Meppen; Barbara Pacini; Steven Harper; Annalise Di Marco; Fabrizio Fiore; Claudio Giuliano; Vincenzo Pucci; Ralph Laufer; Nadia Gennari; Isabella Marcucci; Joseph F Leone; David B Olsen; Malcolm MacCoss; Michael Rowley; Frank Narjes
Phosphoramidate prodrugs of 2'-C-methylcytidine for therapy of hepatitis C virus infection.
Journal of medicinal chemistry 2009;52(17):5394-407.
2009: Malte Meppen; Barbara Pacini; Renzo Bazzo; Uwe Koch; Joseph F Leone; Kenneth A Koeplinger; Michael Rowley; Sergio Altamura; Annalise Di Marco; Fabrizio Fiore; Claudio Giuliano; Odalys Gonzalez Paz; Ralph Laufer; Vincenzo Pucci; Frank Narjes; Cristina Gardelli
Cyclic phosphoramidates as prodrugs of 2'-C-methylcytidine.
European journal of medicinal chemistry 2009;44(9):3765-70.
2009: 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; Andrea Carfì
Identification and biological evaluation of a series of 1H-benzo[de]isoquinoline-1,3(2H)-diones as hepatitis C virus NS5B polymerase inhibitors.
Journal of medicinal chemistry 2009;52(16):5217-27.
2009: Immacolata Conte; Claudio Giuliano; Caterina Ercolani; Frank Narjes; Uwe Koch; Michael Rowley; Sergio Altamura; Raffaele De Francesco; Petra Neddermann; Giovanni Migliaccio; Ian Stansfield
Synthesis and SAR of piperazinyl-N-phenylbenzamides as inhibitors of hepatitis C virus RNA replication in cell culture.
Bioorganic & medicinal chemistry letters 2009;19(6):1779-83.
2009: Monica Donghi; Barbara Attenni; Cristina Gardelli; Annalise Di Marco; Fabrizio Fiore; Claudio Giuliano; Ralph Laufer; Joseph F Leone; Vincenzo Pucci; Michael Rowley; Frank Narjes
Synthesis and evaluation of novel phosphoramidate prodrugs of 2'-methyl cytidine as inhibitors of hepatitis C virus NS5B polymerase.
Bioorganic & medicinal chemistry letters 2009;19(5):1392-5.
2009: Ian Stansfield; Caterina Ercolani; Angela Mackay; Immacolata Conte; Marco Pompei; Uwe Koch; Nadia Gennari; Claudio Giuliano; Michael Rowley; Frank Narjes
Tetracyclic indole inhibitors of hepatitis C virus NS5B-polymerase.
Bioorganic & medicinal chemistry letters 2009;19(3):627-32.
2009: Jörg Habermann; Elena Capitò; Maria del Rosario Rico Ferreira; Uwe Koch; Frank Narjes
Discovery of pentacyclic compounds as potent inhibitors of hepatitis C virus NS5B RNA polymerase.
Bioorganic & medicinal chemistry letters 2009;19(3):633-8.
2009: Mariana Gallo; Matteo Pennestri; Matthew James Bottomley; Gaetano Barbato; Tommaso Eliseo; Maurizio Paci; Frank Narjes; Raffaele De Francesco; Vincenzo Summa; Uwe Koch; Renzo Bazzo; Daniel O Cicero
Binding of a noncovalent inhibitor exploiting the S' region stabilizes the hepatitis C virus NS3 protease conformation in the absence of cofactor.
Journal of molecular biology 2009;385(4):1142-55.
2007: Ian Stansfield; Marco Pompei; Immacolata Conte; Caterina Ercolani; Giovanni Migliaccio; Mark Jairaj; Claudio Giuliano; Michael Rowley; Frank Narjes
Development of carboxylic acid replacements in indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase.
Bioorganic & medicinal chemistry letters 2007;17(18):5143-9.
2007: Uwe Koch; Frank Narjes
Recent progress in the development of inhibitors of the hepatitis C virus RNA-dependent RNA polymerase.
Current topics in medicinal chemistry 2007;7(13):1302-29.
2006: Jesus M Ontoria; Jose I Martìn Hernando; Savina Malancona; Barbara Attenni; Ian Stansfield; Immacolata Conte; Caterina Ercolani; Jörg Habermann; Simona Ponzi; Marcello Di Filippo; Uwe Koch; Michael Rowley; Frank Narjes
Identification of thieno[3,2-b]pyrroles as allosteric inhibitors of hepatitis C virus NS5B polymerase.
Bioorganic & medicinal chemistry letters 2006;16(15):4026-30.
2006: Uwe Koch; Barbara Attenni; Savina Malancona; Stefania Colarusso; Immacolata Conte; Marcello Di Filippo; Steven Harper; Barbara Pacini; Claudia Giomini; Steven Thomas; Ilario Incitti; Licia tomei; Raffaele De Francesco; Sergio Altamura; Victor G Matassa; Frank Narjes
2-(2-Thienyl)-5,6-dihydroxy-4-carboxypyrimidines as inhibitors of the hepatitis C virus NS5B polymerase: discovery, SAR, modeling, and mutagenesis.
Journal of medicinal chemistry 2006;49(5):1693-705.
2006: Uwe Koch; Frank Narjes
Allosteric inhibition of the hepatitis C virus NS5B RNA dependent RNA polymerase.
Infectious disorders drug targets 2006;6(1):31-41.
2005: Claudio Giuliano; F Fiore; Annalise Di Marco; J Padron Velazquez; A Bishop; Fabio Bonelli; Odalys Gonzalez Paz; Isabella Marcucci; Steven Harper; Frank Narjes; Barbara Pacini; Edith Monteagudo; Giovanni Migliaccio; Michael Rowley; Ralph Laufer
Preclinical pharmacokinetics and metabolism of a potent non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
Xenobiotica; the fate of foreign compounds in biological systems 2005;35(10-11):1035-54.
2005: Stefania Di Marco; Cinzia Volpari; Licia tomei; Sergio Altamura; Steven Harper; Frank Narjes; Uwe Koch; Michael Rowley; Raffaele De Francesco; Giovanni Migliaccio; Andrea Carfí
Interdomain communication in hepatitis C virus polymerase abolished by small molecule inhibitors bound to a novel allosteric site.
The Journal of biological chemistry 2005;280(33):29765-70.
2005: Steven Harper; Salvatore Avolio; Barbara Pacini; Marcello Di Filippo; Sergio Altamura; Licia tomei; Giacomo Paonessa; Stefania Di Marco; Andrea Carfi; Claudio Giuliano; Julio Padron; Fabio Bonelli; Giovanni Migliaccio; Raffaele De Francesco; Ralph Laufer; Michael Rowley; Frank Narjes
Potent inhibitors of subgenomic hepatitis C virus RNA replication through optimization of indole-N-acetamide allosteric inhibitors of the viral NS5B polymerase.
Journal of medicinal chemistry 2005;48(14):4547-57.
2005: Steven Harper; Barbara Pacini; Salvatore Avolio; Marcello Di Filippo; Giovanni Migliaccio; Ralph Laufer; Raffaele De Francesco; Michael Rowley; Frank Narjes
Development and preliminary optimization of indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase.
Journal of medicinal chemistry 2005;48(5):1314-7.
2004: Ian Stansfield; Salvatore Avolio; Stefania Colarusso; Nadia Gennari; Frank Narjes; Barbara Pacini; Simona Ponzi; Steven Harper
Active site inhibitors of HCV NS5B polymerase. The development and pharmacophore of 2-thienyl-5,6-dihydroxypyrimidine-4-carboxylic acid.
Bioorganic & medicinal chemistry letters 2004;14(20):5085-8.
2004: Savina Malancona; Stefania Colarusso; Jesus M Ontoria; Antonella Marchetti; Marco Poma; Ian Stansfield; Ralph Laufer; Annalise Di Marco; Marina Taliani; Maria Verdirame; Odalys Gonzalez Paz; Victor G Matassa; Frank Narjes
SAR and pharmacokinetic studies on phenethylamide inhibitors of the hepatitis C virus NS3/NS4A serine protease.
Bioorganic & medicinal chemistry letters 2004;14(17):4575-9.
2004: Emanuela Nizi; Uwe Koch; Jesus M Ontoria; Antonella Marchetti; Frank Narjes; Savina Malancona; Victor G Matassa; Cristina Gardelli
Capped dipeptide phenethylamide inhibitors of the HCV NS3 protease.
Bioorganic & medicinal chemistry letters 2004;14(9):2151-4.
2003: Licia tomei; Sergio Altamura; Linda Bartholomew; Antonino Biroccio; Alessandra Ceccacci; Laura Pacini; Frank Narjes; Nadia Gennari; Monica Bisbocci; Ilario Incitti; Laura Orsatti; Steven Harper; Ian Stansfield; Michael Rowley; Raffaele De Francesco; Giovanni Migliaccio
Mechanism of action and antiviral activity of benzimidazole-based allosteric inhibitors of the hepatitis C virus RNA-dependent RNA polymerase.
Journal of virology 2003;77(24):13225-31.
2003: Caterina Trozzi; Linda Bartholomew; Alessandra Ceccacci; Gabriella Biasiol; Laura Pacini; Sergio Altamura; Frank Narjes; Ester Muraglia; Giacomo Paonessa; Uwe Koch; Raffaele De Francesco; Christian Steinkuhler; Giovanni Migliaccio
In vitro selection and characterization of hepatitis C virus serine protease variants resistant to an active-site peptide inhibitor.
Journal of virology 2003;77(6):3669-79.
2003: Frank Narjes; Uwe Koch; Christian Steinkühler
Recent developments in the discovery of hepatitis C virus serine protease inhibitors--towards a new class of antiviral agents?
Expert opinion on investigational drugs 2003;12(2):153-63.
2003: Stefania Colarusso; Uwe Koch; Benjamin Gerlach; Christian Steinkühler; Raffaele De Francesco; Sergio Altamura; Victor G Matassa; Frank Narjes
Phenethyl amides as novel noncovalent inhibitors of hepatitis C virus NS3/4A protease: discovery, initial SAR, and molecular modeling.
Journal of medicinal chemistry 2003;46(3):345-8.
2002: Stefania Colarusso; Benjamin Gerlach; Uwe Koch; Ester Muraglia; Immacolata Conte; Ian Stansfield; Victor G Matassa; Frank Narjes
Evolution, synthesis and SAR of tripeptide alpha-ketoacid inhibitors of the hepatitis C virus NS3/NS4A serine protease.
Bioorganic & medicinal chemistry letters 2002;12(4):705-8.
2002: Frank Narjes; Koehler F Konrad; Uwe Koch; Benjamin Gerlach; Stefania Colarusso; Christian Steinkühler; Mirko Brunetti; Sergio Altamura; Raffaele De Francesco; Victor G Matassa
A designed P1 cysteine mimetic for covalent and non-covalent inhibitors of HCV NS3 protease.
Bioorganic & medicinal chemistry letters 2002;12(4):701-4.
2001: Michele Pallaoro; Armin Lahm; Gabriella Biasiol; Mirko Brunetti; Caterina Nardella; Laura Orsatti; Fabio Bonelli; Stefania Orrù; Frank Narjes; Christian Steinkühler
Characterization of the hepatitis C virus NS2/3 processing reaction by using a purified precursor protein.
Journal of virology 2001;75(20):9939-46.
2001: Christian Steinkühler; Uwe Koch; Frank Narjes; Victor G Matassa
Hepatitis C virus protease inhibitors: current progress and future challenges.
Current medicinal chemistry 2001;8(8):919-932.
2000: Daniela Fattori; A Urbani; Mirko Brunetti; Raffaele Ingenito; Antonello Pessi; K Prendergast; Frank Narjes; Victor G Matassa; Raffaele De Francesco; Christian Steinkühler
Probing the active site of the hepatitis C virus serine protease by fluorescence resonance energy transfer.
The Journal of biological chemistry 2000;275(20):15106-13.
2000: Gaetano Barbato; Daniel O Cicero; Florence Cordier; Frank Narjes; Benjamin Gerlach; Sonia Sambucini; Stephan Grzesiek; Victor G Matassa; Raffaele De Francesco; Renzo Bazzo
Inhibitor binding induces active site stabilization of the HCV NS3 protein serine protease domain.
The EMBO journal 2000;19(6):1195-206.
2000: Stefania Di Marco; M Rizzi; Cinzia Volpari; Martin A Walsh; Frank Narjes; Stefania Colarusso; Raffaele De Francesco; Victor G Matassa; maurizio sollazzo
Inhibition of the hepatitis C virus NS3/4A protease. The crystal structures of two protease-inhibitor complexes.
The Journal of biological chemistry 2000;275(10):7152-7.
2000: Frank Narjes; Mirko Brunetti; Stefania Colarusso; Benjamin Gerlach; Uwe Koch; Gabriella Biasiol; Daniela Fattori; Raffaele De Francesco; Victor G Matassa; Christian Steinkühler
Alpha-ketoacids are potent slow binding inhibitors of the hepatitis C virus NS3 protease.
Biochemistry 2000;39(7):1849-61.
1997: A Urbani; Elisabetta Bianchi; Frank Narjes; Anna Tramontano; Raffaele De Francesco; Christian Steinkühler; Antonello Pessi
Substrate specificity of the hepatitis C virus serine protease NS3.
The Journal of biological chemistry 1997;272(14):9204-9.