Peer-reviewed veterinary case report
2-(Isopropylamino)thieno[3,2-d]pyrimidin-4(3H)-one derivatives as selective phosphodiesterase 7 inhibitors with potent in vivo efficacy.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2015
- Authors:
- Endo, Yusuke et al.
- Affiliation:
- Drug Research Center · Japan
Abstract
A new series of thienopyrimidinones is synthesized and evaluated as selective phosphodiesterase 7 (PDE7) inhibitors for the treatment of inflammatory diseases. The modification of the substituents on thienopyrimidinone revealed that an isopropylamino group at the 2-position was favorable for aqueous solubility. The introduction of 3-pyrrolidines at the 7-position resulted in good solubility, highly potent activity, and good PDE7 selectivity. Among the synthesized compounds, compound 46 exhibited the greatest inhibition of ear edema in a phorbol ester-induced mouse model.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/25866242/