Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594106 | Bioorganic & Medicinal Chemistry Letters | 2011 | 6 Pages |
Abstract
A structural survey of pyrazolopyridine-pyridazinone phosphodiesterase (PDE) inhibitors was made with a view to optimization of their dual PDE3/4-inhibitory activity for respiratory disease applications. These studies identified (â)-6-(7-methoxy-2-trifluoromethylpyrazolo[1,5-a]pyridine-4-yl)-5-methyl-4,5-dihydro-3-(2H)-pyridazinone (KCA-1490, compound 2ac) as a compound with potent combined bronchodilatory and anti-inflammatory activity and an improved therapeutic window over roflumilast.
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Authors
Koji Ochiai, Naoki Ando, Kazuhiko Iwase, Tetsuya Kishi, Kazunori Fukuchi, Akira Ohinata, Hitomi Zushi, Tokutaro Yasue, David R. Adams, Yasushi Kohno,