Phthalazine PDE4 inhibitors. Part 3: The synthesis and in vitro evaluation of derivatives with a hydrogen bond acceptor

M Napoletano, G Norcini, F Pellacini, F Marchini…

文献索引：Napoletano, Mauro; Norcini, Gabriele; Pellacini, Franco; Marchini, Francesco; Morazzoni, Gabriele; Fattori, Raimondo; Ferlenga, Pierpaolo; Pradella, Lorenzo Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 1 p. 5 - 8

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被引用次数: 13

摘要

This communication describes the synthesis and in vitro evaluation of a novel and potent series of phthalazine phosphodiesterase type (IV)(PDE4) inhibitors. The interaction with two distinct polar binding sites allowed us to eliminate the cyclopentyloxy substitution from rolipram-like analogues.