Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents

…, A Hatzelmann, M Van Slingerland…

Index: Van der Mey, Margaretha; Bommele, Kirsten M.; Boss, Hildegard; Hatzelmann, Armin; Van Slingerland, Mike; Sterk, Geert J.; Timmerman, Hendrik Journal of Medicinal Chemistry, 2003 , vol. 46, # 10 p. 2008 - 2016

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Citation Number: 51

Abstract

In this study, the synthesis and in vitro and in vivo pharmacological investigations of a new series of phthalazinone/pyridazinone hybrids with both PDE3 and PDE4 inhibitory activities are described. These compounds combine the pharmacophores of recently discovered 4a, 5, 8, 8a-tetrahydro-2 H-phthalazin-1-one-type inhibitors of PDE4 and the well-known 2 H- pyridazin-3-one-type PDE3 inhibitors such as the tetrahydrobenzimidazoles. Most of the ...