roflumilast and Inflammation

roflumilast has been researched along with Inflammation* in 1 studies

Other Studies

1 other study(ies) available for roflumilast and Inflammation

Article	Year
Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases. Journal of medicinal chemistry, 2017, 07-13, Volume: 60, Issue:13 The anti-inflammatory potential of p38 mitogen-activated protein kinase (MAPK) inhibitors was coincidentally expanded to a dual inhibition of p38α MAPK and phosphodiesterase 4 (PDE4), and the potential benefits arising from the blockage of both inflammation-related enzymes were thoroughly investigated. The most promising compound, CBS-3595 (1), was successively evaluated in in vitro experiments as well as in ex vivo and in vivo preclinical studies after administration of 1 to rodents, dogs, and monkeys. The resulting data clearly indicated a potent suppression of tumor necrosis factor alpha release. For reconfirming the findings of the animal studies when administering 1 to healthy human volunteers, a phase I clinical trial was conducted. Apart from further information regarding the pharmacokinetic and pharmacodynamic characteristics of 1, it was demonstrated that dual inhibition of p38α MAPK and PDE4 is able to synergistically attenuate the excessive anti-inflammatory response. Topics: Aminopyridines; Animals; Anti-Inflammatory Agents, Non-Steroidal; Chronic Disease; Cyclic Nucleotide Phosphodiesterases, Type 4; Drug Discovery; Humans; Imidazoles; Inflammation; Mitogen-Activated Protein Kinase 14; Phosphodiesterase 4 Inhibitors; Protein Kinase Inhibitors; Tumor Necrosis Factor-alpha	2017

Article

Year

Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases.

Journal of medicinal chemistry, 2017, 07-13, Volume: 60, Issue:13

The anti-inflammatory potential of p38 mitogen-activated protein kinase (MAPK) inhibitors was coincidentally expanded to a dual inhibition of p38α MAPK and phosphodiesterase 4 (PDE4), and the potential benefits arising from the blockage of both inflammation-related enzymes were thoroughly investigated. The most promising compound, CBS-3595 (1), was successively evaluated in in vitro experiments as well as in ex vivo and in vivo preclinical studies after administration of 1 to rodents, dogs, and monkeys. The resulting data clearly indicated a potent suppression of tumor necrosis factor alpha release. For reconfirming the findings of the animal studies when administering 1 to healthy human volunteers, a phase I clinical trial was conducted. Apart from further information regarding the pharmacokinetic and pharmacodynamic characteristics of 1, it was demonstrated that dual inhibition of p38α MAPK and PDE4 is able to synergistically attenuate the excessive anti-inflammatory response.

Topics: Aminopyridines; Animals; Anti-Inflammatory Agents, Non-Steroidal; Chronic Disease; Cyclic Nucleotide Phosphodiesterases, Type 4; Drug Discovery; Humans; Imidazoles; Inflammation; Mitogen-Activated Protein Kinase 14; Phosphodiesterase 4 Inhibitors; Protein Kinase Inhibitors; Tumor Necrosis Factor-alpha

2017