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Eur J Med Chem. 2011 Oct;46(10):4946-56. doi: 10.1016/j.ejmech.2011.07.054. Epub 2011 Aug 5.

Synthesis and biological activity of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel and potent phosphodiesterase type 4 inhibitors.

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Department of Medicinal Chemistry, Almirall S.A., R&D Centre, Laureà Miró 408-410, 08980 Sant Feliu de Llobregat, Catalonia, Spain.


A series of pyrido[3',2':4,5]furo[3,2-d]pyrimidines (PFP) were synthesized and tested for phosphodiesterase type 4 (PDE4) inhibitory activity, with the potential to treat asthma and chronic obstructive pulmonary disease (COPD). Structure-activity relationships within this series, leading to an increase of potency on the enzyme, is presented. Both gem-dimethylcyclohexyl moieties fused to the pyridine ring and the substitution at the 5 position of the PFP scaffold, proved to be key elements in order to get a high affinity in the enzyme.

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