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

Mauro Napoletano, Gabriele Norcini, Franco Pellacini, Francesco Marchini, Gabriele Morazzoni, Raimondo Fattori, Pierpaolo Ferlenga, Lorenzo Pradella

Research output: Contribution to journalArticle

Abstract

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.

Original languageEnglish
Pages (from-to)5-8
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume12
Issue number1
DOIs
Publication statusPublished - Jan 7 2002

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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  • Cite this

    Napoletano, M., Norcini, G., Pellacini, F., Marchini, F., Morazzoni, G., Fattori, R., Ferlenga, P., & Pradella, L. (2002). Phthalazine PDE4 inhibitors. Part 3: The synthesis and in vitro evaluation of derivatives with a hydrogen bond acceptor. Bioorganic and Medicinal Chemistry Letters, 12(1), 5-8. https://doi.org/10.1016/S0960-894X(01)00668-0