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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.

A series of 6-aryl-4,5-heterocyclic-fused pyridazinones were designed and synthesized as selective phosphodiesterase (PDE) IV inhibitors. Biological evaluation of these compounds demonstrated a good selectivity profile toward the PDE IV family and greatly attenuated affinity for the Rolipram high-affinity binding site that seems to be responsible for undesiderable side effects. Structure-activity relationships (SARs) studies showed that the presence of an ethyl group at pyridazine N-2 is associated with the best potency and selectivity profile.[1]

References

  1. Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors. Dal Piaz, V., Giovannoni, M.P., Castellana, C., Palacios, J.M., Beleta, J., Doménech, T., Segarra, V. J. Med. Chem. (1997) [Pubmed]
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