benzofurans and pyrazolopyridine

benzofurans has been researched along with pyrazolopyridine* in 1 studies

Other Studies

1 other study(ies) available for benzofurans and pyrazolopyridine

Article	Year
Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents. Bioorganic & medicinal chemistry letters, 2008, Mar-15, Volume: 18, Issue:6 Potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE) were discovered with several new heterocyclic P1' groups in conjunction with cyclic beta-amino hydroxamic acid scaffolds. Among them, the pyrazolopyridine provided the best overall profile when combined with tetrahydropyran beta-amino hydroxamic acid scaffold. Specifically, inhibitor 49 showed IC(50) value of 1 nM against porcine TACE and 170 nM in the suppression of LPS-induced TNF-alpha of human whole blood. Compound 49 also displayed excellent selectivity over a wide panel of MMPs as well as excellent oral bioavailability (F%>90%) in rat n-in-1 PK studies. Topics: ADAM Proteins; ADAM17 Protein; Administration, Oral; Animals; Benzofurans; Biological Availability; Humans; Hydroxamic Acids; Imidazoles; Indoles; Lipopolysaccharides; Matrix Metalloproteinase Inhibitors; Molecular Structure; Protease Inhibitors; Pyrazoles; Pyridines; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Tumor Necrosis Factor-alpha	2008

Article

Year

Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents.

Bioorganic & medicinal chemistry letters, 2008, Mar-15, Volume: 18, Issue:6

Potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE) were discovered with several new heterocyclic P1' groups in conjunction with cyclic beta-amino hydroxamic acid scaffolds. Among them, the pyrazolopyridine provided the best overall profile when combined with tetrahydropyran beta-amino hydroxamic acid scaffold. Specifically, inhibitor 49 showed IC(50) value of 1 nM against porcine TACE and 170 nM in the suppression of LPS-induced TNF-alpha of human whole blood. Compound 49 also displayed excellent selectivity over a wide panel of MMPs as well as excellent oral bioavailability (F%>90%) in rat n-in-1 PK studies.

Topics: ADAM Proteins; ADAM17 Protein; Administration, Oral; Animals; Benzofurans; Biological Availability; Humans; Hydroxamic Acids; Imidazoles; Indoles; Lipopolysaccharides; Matrix Metalloproteinase Inhibitors; Molecular Structure; Protease Inhibitors; Pyrazoles; Pyridines; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Tumor Necrosis Factor-alpha

2008