PubRank

F George Njoroge

Author PubWeight™ 38.87‹?›

Top papers

Rank Title Journal Year PubWeight™‹?›
1 Discovery of (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]- 3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor: a potential therapeutic agent for the treatment of hepatitis C infection. J Med Chem 2006 2.09
2 Characterization of resistance mutations against HCV ketoamide protease inhibitors. Antiviral Res 2007 1.55
3 Mutations conferring resistance to SCH6, a novel hepatitis C virus NS3/4A protease inhibitor. Reduced RNA replication fitness and partial rescue by second-site mutations. J Biol Chem 2005 1.54
4 A review of HCV protease inhibitors. Curr Opin Investig Drugs 2009 1.39
5 Discovery of the HCV NS3/4A protease inhibitor (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3- [2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (Sch 503034) II. Key steps in structure-based optimization. J Med Chem 2007 1.21
6 Impact of naturally occurring variants of HCV protease on the binding of different classes of protease inhibitors. Biochemistry 2006 0.94
7 The Journey to the Discovery of Boceprevir: an NS3-NS4 HCV protease inhibitor for the treatment of chronic hepatitis C. Prog Med Chem 2010 0.87
8 Regioselective cobalt-catalyzed addition of sulfides to unactivated alkenes. J Org Chem 2011 0.87
9 Discovery of potent sulfonamide P4-capped ketoamide second generation inhibitors of hepatitis C virus NS3 serine protease with favorable pharmacokinetic profiles in preclinical species. Bioorg Med Chem 2010 0.86
10 In vitro antiviral activity of SCH446211 (SCH6), a novel inhibitor of the hepatitis C virus NS3 serine protease. J Antimicrob Chemother 2006 0.84
11 Correlation between PAMPA permeability and cellular activities of hepatitis C virus protease inhibitors. Biochem Pharmacol 2007 0.84
12 Toward the back-up of boceprevir (SCH 503034): discovery of new extended P4-capped ketoamide inhibitors of hepatitis C virus NS3 serine protease with improved potency and pharmacokinetic profiles. J Med Chem 2009 0.83
13 Toward second generation hepatitis C virus NS3 serine protease inhibitors: discovery of novel P4 modified analogues with improved potency and pharmacokinetic profile. J Med Chem 2009 0.82
14 Discovery of SCH446211 (SCH6): a new ketoamide inhibitor of the HCV NS3 serine protease and HCV subgenomic RNA replication. J Med Chem 2006 0.82
15 Structure-activity relationship (SAR) optimization of 6-(indol-2-yl)pyridine-3-sulfonamides: identification of potent, selective, and orally bioavailable small molecules targeting hepatitis C (HCV) NS4B. J Med Chem 2013 0.82
16 Synthesis of new 4,5-dihydrofuranoindoles and their evaluation as HCV NS5B polymerase inhibitors. Org Lett 2012 0.82
17 Cyclic sulfones as novel P3-caps for hepatitis C virus NS3/4A (HCV NS3/4A) protease inhibitors: synthesis and evaluation of inhibitors with improved potency and pharmacokinetic profiles. J Med Chem 2010 0.82
18 A novel class of highly potent irreversible hepatitis C virus NS5B polymerase inhibitors. J Med Chem 2012 0.82
19 Novel dipeptide macrocycles from 4-oxo, -thio, and -amino-substituted proline derivatives. J Org Chem 2002 0.81
20 Discovery and structure-activity relationship of P1-P3 ketoamide derived macrocyclic inhibitors of hepatitis C virus NS3 protease. J Med Chem 2009 0.81
21 P2-P4 macrocyclic inhibitors of hepatitis C virus NS3-4A serine protease. Bioorg Med Chem Lett 2006 0.80
22 Potent ketoamide inhibitors of HCV NS3 protease derived from quaternized P1 groups. Bioorg Med Chem Lett 2010 0.80
23 Application of ring-closing metathesis for the synthesis of macrocyclic peptidomimetics as inhibitors of HCV NS3 protease. Org Lett 2007 0.80
24 Second-generation highly potent and selective inhibitors of the hepatitis C virus NS3 serine protease. J Med Chem 2009 0.80
25 Structure-activity relationship (SAR) development and discovery of potent indole-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase. J Med Chem 2012 0.80
26 Synthesis and biological activity of macrocyclic inhibitors of hepatitis C virus (HCV) NS3 protease. Bioorg Med Chem Lett 2005 0.79
27 The introduction of P4 substituted 1-methylcyclohexyl groups into Boceprevir: a change in direction in the search for a second generation HCV NS3 protease inhibitor. Bioorg Med Chem Lett 2010 0.78
28 Potent 7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid-based macrocyclic inhibitors of hepatitis C virus NS3 protease. J Med Chem 2006 0.78
29 Macrocyclic inhibitors of HCV NS3 protease. Expert Opin Ther Pat 2009 0.77
30 Novel inhibitors of hepatitis C NS3-NS4A serine protease derived from 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid. Bioorg Med Chem Lett 2006 0.77
31 Macrocyclic inhibitors of HCV NS3-4A protease: design and structure activity relationship. Curr Top Med Chem 2007 0.77
32 Ultra-performance liquid chromatography/tandem mass spectrometric determination of diastereomers of SCH 503034 in monkey plasma. J Chromatogr B Analyt Technol Biomed Life Sci 2007 0.77
33 Discovery of novel HCV inhibitors: synthesis and biological activity of 6-(indol-2-yl)pyridine-3-sulfonamides targeting hepatitis C virus NS4B. Bioorg Med Chem Lett 2013 0.77
34 Design and synthesis of depeptidized macrocyclic inhibitors of hepatitis C NS3-4A protease using structure-based drug design. J Med Chem 2005 0.77
35 5-Benzothiazole substituted pyrimidine derivatives as HCV replication (replicase) inhibitors. Bioorg Med Chem Lett 2012 0.77
36 Potent and selective small molecule NS3 serine protease inhibitors of Hepatitis C virus with dichlorocyclopropylproline as P2 residue. Bioorg Med Chem 2007 0.77
37 Design, synthesis, and evaluation of oxygen-containing macrocyclic peptidomimetics as inhibitors of HCV NS3 protease. J Med Chem 2009 0.77
38 Discovery of an irreversible HCV NS5B polymerase inhibitor. Bioorg Med Chem Lett 2013 0.76
39 Non-peptidic small-molecule inhibitors of the single-chain hepatitis C virus NS3 protease/NS4A cofactor complex discovered by structure-based NMR screening. J Med Chem 2004 0.76
40 Novel potent inhibitors of hepatitis C virus (HCV) NS3 protease with cyclic sulfonyl P3 cappings. Bioorg Med Chem Lett 2009 0.76
41 Lead Optimization in Discovery Drug Metabolism and Pharmacokinetics/Case study: The Hepatitis C Virus (HCV) Protease Inhibitor SCH 503034. Perspect Medicin Chem 2007 0.75
42 Key steps in the structure-based optimization of the hepatitis C virus NS3/4A protease inhibitor SCH503034. J Synchrotron Radiat 2008 0.75
43 Depeptidization efforts on P3-P2' alpha-ketoamide inhibitors of HCV NS3-4A serine protease: effect on HCV replicon activity. Bioorg Med Chem Lett 2006 0.75
44 Novel potent hepatitis C virus NS3 serine protease inhibitors derived from proline-based macrocycles. J Med Chem 2006 0.75
45 Design, synthesis, and biological activity of m-tyrosine-based 16- and 17-membered macrocyclic inhibitors of hepatitis C virus NS3 serine protease. J Med Chem 2005 0.75
46 Novel inhibitors of the hepatitis C virus NS3 proteinase. Bioorg Med Chem Lett 2005 0.75
47 A convenient synthesis of cis and trans 4-tert-butoxycarbonyl-substituted cyclohexylglycine. J Org Chem 2002 0.75
48 Syntheses of novel 4-tert-alkyl ether proline-based 16- and 17-membered macrocyclic compounds. J Org Chem 2002 0.75
49 Permeability evaluation of peptidic HCV protease inhibitors in Caco-2 cells-correlation with in vivo absorption predicted in humans. Biochem Pharmacol 2008 0.75
50 The role of P-glycoprotein in the pharmacokinetics and tissue distribution of a hepatitis C virus protease inhibitor. Drug Metab Lett 2009 0.75
51 Proline-based macrocyclic inhibitors of the hepatitis C virus: stereoselective synthesis and biological activity. Angew Chem Int Ed Engl 2005 0.75
52 Discovery of N-(6-Fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide (LSN 3213128), a Potent and Selective Non-Classical Antifolate Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase (AICARFT) Inhibitor Effective at Tumor Suppression in a Cancer Xenograft Model. J Med Chem 2017 0.75
53 Application of ruthenium-induced macrocyclization for the construction of macrocyclic depsipeptides. J Org Chem 2002 0.75
54 Towards the second generation of Boceprevir: Dithianes as an alternative P2 substituent for 2,2-dimethyl cycloproyl proline in HCV NS3 protease inhibitors. Bioorg Med Chem Lett 2010 0.75
55 Synthesis and SAR of pyridothiazole substituted pyrimidine derived HCV replication inhibitors. Bioorg Med Chem Lett 2012 0.75
56 Discovery of novel tricyclic indole derived inhibitors of HCV NS5B RNA dependent RNA polymerase. Bioorg Med Chem 2013 0.75
57 Novel 2-oxoimidazolidine-4-carboxylic acid derivatives as hepatitis C virus NS3-4A serine protease inhibitors: synthesis, activity, and X-ray crystal structure of an enzyme inhibitor complex. Bioorg Med Chem Lett 2004 0.75
58 Synthesis and SAR of geminal substitutions at the C5' carbosugar position of pyrimidine-derived HCV inhibitors. Bioorg Med Chem Lett 2012 0.75
59 Stereoselective synthesis of beta-substituted beta-amino sulfones and sulfonamides via addition of sulfonyl anions to chiral N-sulfinyl imines. Org Lett 2006 0.75