roflumilast and apremilast

roflumilast has been researched along with apremilast* in 1 studies

Other Studies

1 other study(ies) available for roflumilast and apremilast

Article	Year
Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor. Journal of medicinal chemistry, 2009, Mar-26, Volume: 52, Issue:6 In this communication, we report the discovery of 1S (apremilast), a novel potent and orally active phosphodiesterase 4 (PDE4) and tumor necrosis factor-alpha inhibitor. The optimization of previously reported 3-(1,3-dioxo-1,3-dihydroisoindol-2-yl)-3-(3,4-dimethoxyphenyl)propionic acid PDE4 inhibitors led to this series of sulfone analogues. Evaluation of the structure-activity relationship of substitutions on the phthalimide group led to the discovery of an acetylamino analogue 1S, which is currently in clinical trials. Topics: Administration, Oral; Animals; Drug Discovery; Humans; Phosphodiesterase 4 Inhibitors; Phosphodiesterase Inhibitors; Rats; Stereoisomerism; Structure-Activity Relationship; Thalidomide; Tumor Necrosis Factor-alpha	2009

Article

Year

Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor.

Journal of medicinal chemistry, 2009, Mar-26, Volume: 52, Issue:6

In this communication, we report the discovery of 1S (apremilast), a novel potent and orally active phosphodiesterase 4 (PDE4) and tumor necrosis factor-alpha inhibitor. The optimization of previously reported 3-(1,3-dioxo-1,3-dihydroisoindol-2-yl)-3-(3,4-dimethoxyphenyl)propionic acid PDE4 inhibitors led to this series of sulfone analogues. Evaluation of the structure-activity relationship of substitutions on the phthalimide group led to the discovery of an acetylamino analogue 1S, which is currently in clinical trials.

Topics: Administration, Oral; Animals; Drug Discovery; Humans; Phosphodiesterase 4 Inhibitors; Phosphodiesterase Inhibitors; Rats; Stereoisomerism; Structure-Activity Relationship; Thalidomide; Tumor Necrosis Factor-alpha

2009