| Rank |
Title |
Journal |
Year |
PubWeight™‹?› |
|
1
|
Challenges in modern drug discovery: a case study of boceprevir, an HCV protease inhibitor for the treatment of hepatitis C virus infection.
|
Acc Chem Res
|
2008
|
1.14
|
|
2
|
Asymmetric synthesis of 4,4-disubstituted-2-imidazoli-dinones: potent NK1 antagonists.
|
Org Lett
|
2003
|
0.86
|
|
3
|
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
|
|
4
|
Cyclic urea derivatives as potent NK1 selective antagonists.
|
Bioorg Med Chem Lett
|
2005
|
0.85
|
|
5
|
Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions.
|
Bioorg Med Chem Lett
|
2005
|
0.84
|
|
6
|
A novel class of highly potent irreversible hepatitis C virus NS5B polymerase inhibitors.
|
J Med Chem
|
2012
|
0.82
|
|
7
|
The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists.
|
Bioorg Med Chem Lett
|
2005
|
0.82
|
|
8
|
III. Identification of novel CXCR3 chemokine receptor antagonists with a pyrazinyl-piperazinyl-piperidine scaffold.
|
Bioorg Med Chem Lett
|
2011
|
0.82
|
|
9
|
Discovery and structure-activity relationship of P1-P3 ketoamide derived macrocyclic inhibitors of hepatitis C virus NS3 protease.
|
J Med Chem
|
2009
|
0.81
|
|
10
|
Cyclobutane derivatives as potent NK1 selective antagonists.
|
Bioorg Med Chem Lett
|
2006
|
0.81
|
|
11
|
Application of ring-closing metathesis for the synthesis of macrocyclic peptidomimetics as inhibitors of HCV NS3 protease.
|
Org Lett
|
2007
|
0.80
|
|
12
|
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
|
|
13
|
Second-generation highly potent and selective inhibitors of the hepatitis C virus NS3 serine protease.
|
J Med Chem
|
2009
|
0.80
|
|
14
|
The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors.
|
Bioorg Med Chem Lett
|
2009
|
0.80
|
|
15
|
Pharmacological characterization of the novel histamine H3-receptor antagonist N-(3,5-dichlorophenyl)-N'-[[4-(1H-imidazol-4-ylmethyl)phenyl]-methyl]-urea (SCH 79687).
|
J Pharmacol Exp Ther
|
2003
|
0.79
|
|
16
|
Discovery of a series of potent, orally active α,α-disubstituted piperidine NK(1) antagonists.
|
Bioorg Med Chem Lett
|
2010
|
0.78
|
|
17
|
Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine.
|
Bioorg Med Chem Lett
|
2003
|
0.78
|
|
18
|
II. SAR studies of pyridyl-piperazinyl-piperidine derivatives as CXCR3 chemokine antagonists.
|
Bioorg Med Chem Lett
|
2010
|
0.78
|
|
19
|
Triaryl bis-sulfones as cannabinoid-2 receptor ligands: SAR studies.
|
Bioorg Med Chem Lett
|
2005
|
0.78
|
|
20
|
Biaryl substituted hydantoin compounds as TACE inhibitors.
|
Bioorg Med Chem Lett
|
2010
|
0.77
|
|
21
|
5-Benzothiazole substituted pyrimidine derivatives as HCV replication (replicase) inhibitors.
|
Bioorg Med Chem Lett
|
2012
|
0.77
|
|
22
|
Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists.
|
Bioorg Med Chem Lett
|
2005
|
0.77
|
|
23
|
I. Novel HCV NS5B polymerase inhibitors: discovery of indole 2-carboxylic acids with C3-heterocycles.
|
Bioorg Med Chem Lett
|
2011
|
0.77
|
|
24
|
2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors.
|
Bioorg Med Chem Lett
|
2011
|
0.77
|
|
25
|
Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors.
|
Bioorg Med Chem Lett
|
2007
|
0.77
|
|
26
|
Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity.
|
Bioorg Med Chem Lett
|
2002
|
0.76
|
|
27
|
Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands.
|
Bioorg Med Chem Lett
|
2007
|
0.76
|
|
28
|
Non-aromatic A-ring replacement in the triaryl bis-sulfone CB2 receptor inhibitors.
|
Bioorg Med Chem Lett
|
2009
|
0.76
|
|
29
|
Discovery of an irreversible HCV NS5B polymerase inhibitor.
|
Bioorg Med Chem Lett
|
2013
|
0.76
|
|
30
|
SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist.
|
Eur J Pharmacol
|
2002
|
0.76
|
|
31
|
The synthesis of substituted bipiperidine amide compounds as CCR3 ligands: antagonists versus agonists.
|
Bioorg Med Chem Lett
|
2005
|
0.75
|
|
32
|
Discovery of oxazole-based PDE4 inhibitors with picomolar potency.
|
Bioorg Med Chem Lett
|
2012
|
0.75
|
|
33
|
Manipulation of N,O-nucleophilicity: efficient formation of 4-N-substituted 2,4-dihydro-3H-1,2,4-triazolin-3-ones.
|
Org Lett
|
2004
|
0.75
|
|
34
|
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
|
Bioorg Med Chem Lett
|
2010
|
0.75
|
|
35
|
8-Methoxyquinolines as PDE4 inhibitors.
|
Bioorg Med Chem Lett
|
2002
|
0.75
|
|
36
|
Discovery and SAR of hydantoin TACE inhibitors.
|
Bioorg Med Chem Lett
|
2010
|
0.75
|
|
37
|
Discovery of a novel, potent and orally active series of gamma-lactams as selective NK1 antagonists.
|
Bioorg Med Chem Lett
|
2008
|
0.75
|
|
38
|
Benzimidazole-substituted (3-phenoxypropyl)amines as histamine H3 receptor ligands.
|
Bioorg Med Chem Lett
|
2008
|
0.75
|
|
39
|
Synthesis and SAR studies of benzimidazolone derivatives as histamine H3-receptor antagonists.
|
Bioorg Med Chem Lett
|
2013
|
0.75
|
|
40
|
Pyridofuran substituted pyrimidine derivatives as HCV replication (replicase) inhibitors.
|
Bioorg Med Chem Lett
|
2012
|
0.75
|
|
41
|
Development and potential utility of dual and triple NK receptor antagonists.
|
Curr Top Med Chem
|
2003
|
0.75
|
|
42
|
Discovery of novel spirocyclopropyl hydroxamate and carboxylate compounds as TACE inhibitors.
|
Bioorg Med Chem Lett
|
2008
|
0.75
|
|
43
|
II. Novel HCV NS5B polymerase inhibitors: discovery of indole C2 acyl sulfonamides.
|
Bioorg Med Chem Lett
|
2011
|
0.75
|
|
44
|
Potent aza-peptide derived inhibitors of HCV NS3 protease.
|
Bioorg Med Chem Lett
|
2009
|
0.75
|
|
45
|
Discovery of novel tricyclic indole derived inhibitors of HCV NS5B RNA dependent RNA polymerase.
|
Bioorg Med Chem
|
2013
|
0.75
|
|
46
|
Synthesis and profile of SCH351591, a novel PDE4 inhibitor.
|
Bioorg Med Chem Lett
|
2002
|
0.75
|
|
47
|
Synthesis and NK(1)/NK(2) binding activities of a series of diacyl-substituted 2-arylpiperazines.
|
Bioorg Med Chem Lett
|
2002
|
0.75
|
|
48
|
Structure and activity relationships of tartrate-based TACE inhibitors.
|
Bioorg Med Chem Lett
|
2010
|
0.75
|
|
49
|
Novel TNF-α converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases.
|
Bioorg Med Chem Lett
|
2010
|
0.75
|
|
50
|
Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold.
|
Bioorg Med Chem Lett
|
2005
|
0.75
|
|
51
|
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
|
|
52
|
Novel substituted pyrimidines as HCV replication (replicase) inhibitors.
|
Bioorg Med Chem Lett
|
2011
|
0.75
|
|
53
|
Synthesis and SAR of pyridothiazole substituted pyrimidine derived HCV replication inhibitors.
|
Bioorg Med Chem Lett
|
2012
|
0.75
|