201286-79-5Relevant academic research and scientific papers
Orally active indole N-oxide PDE4 inhibitors
Hulme, Christopher,Mathew, Rose,Moriarty, Kevin,Miller, Bruce,Ramanjulu, Mercy,Cox, Paul,Souness, John,Page, Ken M.,Uhl, Joanne,Travis, Jeffrey,Labaudiniere, Richard,Huang, Fu-Chih,Djuric, Stevan W.
, p. 3053 - 3058 (2007/10/03)
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 IC50's 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.
