201286-26-2Relevant articles and documents
The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I
Hulme, Christopher,Moriarty, Kevin,Miller, Bruce,Mathew, Rose,Ramanjulu, Mercy,Cox, Paul,Souness, John,Page, Ken M.,Uhl, Joanne,Travis, Jeffrey,Huang, Fu-Chih,Labaudiniere, Richard,Djuric, Stevan W.
, p. 1867 - 1872 (1998)
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 IC50's for PDEIV inhibition. In vivo activities determined from measurement of serum TNF-α levels in LPS challenged mice (mouse endotoxemia model) are also reported.
