Phosphodiesterase inhibitors. Part 3: Design, synthesis and structure–activity relationships of dual PDE3/4-inhibitory fused bicyclic heteroaromatic- …

…, T Eiraku, A Kojima, K Iwase, T Kishi, K Fukuchi…

Index: Ochiai, Koji; Takita, Satoshi; Eiraku, Tomohiko; Kojima, Akihiko; Iwase, Kazuhiko; Kishi, Tetsuya; Fukuchi, Kazunori; Yasue, Tokutaro; Adams, David R.; Allcock, Robert W.; Jiang, Zhong; Kohno, Yasushi Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 5 p. 1644 - 1658

Full Text: HTML

Citation Number: 28

Abstract

(−)-6-(7-Methoxy-2-trifluoromethylpyrazolo [1, 5-a] pyridin-4-yl)-5-methyl-4, 5-dihydro-3-(2H)- pyridazinone (KCA-1490) is a dual PDE3/4 inhibitor that exhibits potent combined bronchodilatory and anti-inflammatory activity. A survey of potential bicyclic heteroaromatic replacement subunits for the pyrazolo [1, 5-a] pyridine core of KCA-1490 has identified the 4- methoxy-2-(trifluoromethyl) benzo [d] thiazol-7-yl and 8-methoxy-2-(trifluoromethyl) ...