Author/Authors :
Christopher Hulme، نويسنده , , Rose Mathew، نويسنده , , Kevin Moriarty، نويسنده , , Bruce Miller، نويسنده , , Mercy Ramanjulu، نويسنده , , Paul Cox، نويسنده , , John Souness، نويسنده , , Ken M. Page، نويسنده , , Joanne Uhl، نويسنده , , Jeffrey Travis، نويسنده , , Richard Labaudiniere، نويسنده , , Fu-Chih Huang، نويسنده , , Stevan W. Djuric، نويسنده ,
Abstract :
This communication describes the synthesis and in vitro and in vivo evaluation of a novel potent series of phosphodiesterase type (IV) (PDE4) inhibitors. Several of the compounds presented possess low nanomolar IC50ʹs for PDE4 inhibition and excellent in vivo activity for inhibition of TNF-α levels in LPS challenged mice (mouse endotoxemia model). Emesis studies (dog) and efficacy in a SCW arthritis model for the most potent PDE4 inhibitors are presented.
