Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection V Summa, A Petrocchi, F Bonelli, B Crescenzi, M Donghi, M Ferrara, ... Journal of medicinal chemistry 51 (18), 5843-5855, 2008 | 749 | 2008 |
A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase DJ Hazuda, NJ Anthony, RP Gomez, SM Jolly, JS Wai, L Zhuang, ... Proceedings of the National Academy of Sciences 101 (31), 11233-11238, 2004 | 419 | 2004 |
Approaching a new era for hepatitis C virus therapy: inhibitors of the NS3-4A serine protease and the NS5B RNA-dependent RNA polymerase R De Francesco, L Tomei, S Altamura, V Summa, G Migliaccio Antiviral research 58 (1), 1-16, 2003 | 361 | 2003 |
MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants V Summa, SW Ludmerer, JA McCauley, C Fandozzi, C Burlein, G Claudio, ... Antimicrobial agents and chemotherapy 56 (8), 4161-4167, 2012 | 303 | 2012 |
Targeting SARS-CoV-2 proteases and polymerase for COVID-19 treatment: state of the art and future opportunities R Cannalire, C Cerchia, AR Beccari, FS Di Leva, V Summa Journal of medicinal chemistry 65 (4), 2716-2746, 2020 | 211 | 2020 |
Discovery of MK-5172, a macrocyclic hepatitis C virus NS3/4a protease inhibitor S Harper, JA McCauley, MT Rudd, M Ferrara, M DiFilippo, B Crescenzi, ... ACS medicinal chemistry letters 3 (4), 332-336, 2012 | 202 | 2012 |
Discovery of α, γ-diketo acids as potent selective and reversible inhibitors of hepatitis C virus NS5b RNA-dependent RNA polymerase V Summa, A Petrocchi, P Pace, VG Matassa, R De Francesco, S Altamura, ... Journal of medicinal chemistry 47 (1), 14-17, 2004 | 177 | 2004 |
4,5-Dihydroxypyrimidine Carboxamides and N-Alkyl-5-hydroxypyrimidinone Carboxamides Are Potent, Selective HIV Integrase Inhibitors with Good … V Summa, A Petrocchi, VG Matassa, C Gardelli, E Muraglia, M Rowley, ... Journal of medicinal chemistry 49 (23), 6646-6649, 2006 | 147 | 2006 |
HCV NS5b RNA-dependent RNA polymerase inhibitors: from α, γ-diketoacids to 4, 5-dihydroxypyrimidine-or 3-methyl-5-hydroxypyrimidinonecarboxylic acids. Design and synthesis V Summa, A Petrocchi, VG Matassa, M Taliani, R Laufer, R De Francesco, ... Journal of medicinal chemistry 47 (22), 5336-5339, 2004 | 137 | 2004 |
Identification of inhibitors of SARS-CoV-2 3CL-pro enzymatic activity using a small molecule in vitro repurposing screen M Kuzikov, E Costanzi, J Reinshagen, F Esposito, L Vangeel, M Wolf, ... ACS pharmacology & translational science 4 (3), 1096-1110, 2021 | 132 | 2021 |
Synthesis of aryl 2-benzofuranyl and aryl 2-indolyl carbinols of high enantiomeric purity via palladium-catalyzed heteroannulation of chiral arylpropargylic alcohols M Botta, V Summa, F Corelli, G Di Pietro, P Lombardi Tetrahedron: Asymmetry 7 (5), 1263-1266, 1996 | 127 | 1996 |
Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors P Pace, ME Di Francesco, C Gardelli, S Harper, E Muraglia, E Nizi, ... Journal of Medicinal Chemistry 50 (9), 2225-2239, 2007 | 124 | 2007 |
Tetrazole thioacetanilides: potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant E Muraglia, OD Kinzel, R Laufer, MD Miller, G Moyer, V Munshi, F Orvieto, ... Bioorganic & medicinal chemistry letters 16 (10), 2748-2752, 2006 | 119 | 2006 |
Hepatitis C virus NS5A is a direct substrate of casein kinase I-α, a cellular kinase identified by inhibitor affinity chromatography using specific NS5A hyperphosphorylation … M Quintavalle, S Sambucini, V Summa, L Orsatti, F Talamo, ... Journal of Biological Chemistry 282 (8), 5536-5544, 2007 | 116 | 2007 |
Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones C Gardelli, E Nizi, E Muraglia, B Crescenzi, M Ferrara, F Orvieto, P Pace, ... Journal of medicinal chemistry 50 (20), 4953-4975, 2007 | 92 | 2007 |
From dihydroxypyrimidine carboxylic acids to carboxamide HIV-1 integrase inhibitors: SAR around the amide moiety A Petrocchi, U Koch, VG Matassa, B Pacini, KA Stillmock, V Summa Bioorganic & Medicinal Chemistry Letters 17 (2), 350-353, 2007 | 82 | 2007 |
SARS-CoV-2 entry inhibitors: small molecules and peptides targeting virus or host cells R Cannalire, I Stefanelli, C Cerchia, AR Beccari, S Pelliccia, V Summa International Journal of Molecular Sciences 21 (16), 5707, 2020 | 80 | 2020 |
The monoethyl ester of meconic acid is an active site inhibitor of HCV NS5B RNA-dependent RNA polymerase P Pace, E Nizi, B Pacini, S Pesci, V Matassa, R De Francesco, S Altamura, ... Bioorganic & medicinal chemistry letters 14 (12), 3257-3261, 2004 | 80 | 2004 |
Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors E Muraglia, O Kinzel, C Gardelli, B Crescenzi, M Donghi, M Ferrara, E Nizi, ... Journal of medicinal chemistry 51 (4), 861-874, 2008 | 77 | 2008 |
N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase B Crescenzi, C Gardelli, E Muraglia, F Orvieto, P Pace, G Pescatore, ... US Patent 7,169,780, 2007 | 68 | 2007 |