Author/Authors :
Christopher Hulme، نويسنده , , Kevin Moriarty، نويسنده , , Bruce Miller، نويسنده , , Rose Mathew، نويسنده , , Mercy Ramanjulu، نويسنده , , Paul Cox، نويسنده , , John Souness، نويسنده , , Ken M. Page، نويسنده , , Joanne Uhl، نويسنده , , Jeffrey Travis، نويسنده , , Fu-Chih Huang، نويسنده , , Richard Labaudiniere، نويسنده , , Stevan W. Djuric، نويسنده ,
Abstract :
This communication describes the synthesis and in vitro evaluation of a novel potent series of phosphodiesterase type (IV) (PDE4) inhibitors. The compounds described contain an indole moiety which replaces the ‘rolipram-like’ 3-methoxy-4-cyclopentoxy motif. Several of the compounds presented possess low nanomolar IC50ʹs for PDEIV inhibition. In vivo activities determined from measurement of serum TNF-α levels in LPS challenged mice (mouse endotoxemia model) are also reported.
