|
1
|
A novel, orally active CXCR1/2 receptor antagonist, Sch527123, inhibits neutrophil recruitment, mucus production, and goblet cell hyperplasia in animal models of pulmonary inflammation.
|
J Pharmacol Exp Ther
|
2007
|
1.30
|
|
2
|
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
|
J Med Chem
|
2006
|
0.99
|
|
3
|
C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists.
|
Bioorg Med Chem Lett
|
2007
|
0.86
|
|
4
|
Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia.
|
Bioorg Med Chem Lett
|
2011
|
0.80
|
|
5
|
T-type calcium channel blockers: spiro-piperidine azetidines and azetidinones-optimization, design and synthesis.
|
Bioorg Med Chem Lett
|
2010
|
0.77
|
|
6
|
The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia.
|
Bioorg Med Chem Lett
|
2011
|
0.76
|
|
7
|
The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
|
Bioorg Med Chem Lett
|
2012
|
0.76
|
|
8
|
Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists.
|
Bioorg Med Chem Lett
|
2008
|
0.75
|
|
9
|
3,4-Diamino-2,5-thiadiazole-1-oxides as potent CXCR2/CXCR1 antagonists.
|
Bioorg Med Chem Lett
|
2007
|
0.75
|
|
10
|
Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.
|
Bioorg Med Chem Lett
|
2009
|
0.75
|
|
11
|
Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.
|
Bioorg Med Chem Lett
|
2009
|
0.75
|
|
12
|
Synthesis and structure-activity relationships of heteroaryl substituted-3,4-diamino-3-cyclobut-3-ene-1,2-dione CXCR2/CXCR1 receptor antagonists.
|
Bioorg Med Chem Lett
|
2008
|
0.75
|
|
13
|
Design, synthesis, structure-function relationship, bioconversion, and pharmacokinetic evaluation of ertapenem prodrugs.
|
J Med Chem
|
2014
|
0.75
|
|
14
|
Spiro-piperidine azetidinones as potent TRPV1 antagonists.
|
Bioorg Med Chem Lett
|
2008
|
0.75
|