PdCl2-catalyzed synthesis of a new class of isocoumarin derivatives containing aminosulfonyl / aminocarboxamide moiety: First identification of a isocoumarin based PDE4 inhibitor.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113514
Abstract: While anti-inflammatory properties of isocoumarins are known their PDE4 inhibitory potential was not explored previously. In our effort the non-PDE4 inhibitor isocoumarins were transformed into the promising inhibitors via introducing an aminosulfonyl/aminocarboxamide moiety to the… read more here.
Keywords: pde4 inhibitor; aminocarboxamide moiety; moiety; aminosulfonyl aminocarboxamide ... See more keywords
Pharmacology of orismilast, a potent and selective PDE4 inhibitor
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DOI: 10.1111/jdv.18818
Abstract: There remains an unmet need for oral medications that are safe and efficacious for long‐term management of chronic inflammatory skin diseases (CISD). Inhibition of phosphodiesterase 4 (PDE4) can modulate a broad range of pro‐inflammatory cytokines… read more here.
Keywords: pharmacology; pharmacology orismilast; orismilast potent; pde4 ... See more keywords
The PDE4 Inhibitor Tanimilast Blunts Proinflammatory Dendritic Cell Activation by SARS-CoV-2 ssRNAs
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DOI: 10.3389/fimmu.2021.797390
Abstract: Phosphodiesterase 4 (PDE4) inhibitors are immunomodulatory drugs approved to treat diseases associated with chronic inflammatory conditions, such as COPD, psoriasis and atopic dermatitis. Tanimilast (international non-proprietary name of CHF6001) is a novel, potent and selective… read more here.
Keywords: sars cov; activation; dendritic cell; tanimilast ... See more keywords
Acute Lung Functional and Airway Remodeling Effects of an Inhaled Highly Selective Phosphodiesterase 4 Inhibitor in Ventilated Preterm Lambs Exposed to Chorioamnionitis
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DOI: 10.3390/ph16010029
Abstract: Phosphodiesterase (PDE) inhibition has been identified in animal studies as a new treatment option for neonatal lung injury, and as potentially beneficial for early lung development and function. However, our group could show that the… read more here.
Keywords: pde4 inhibitor; inhibitor; lung; chorioamnionitis ... See more keywords