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Bioorg Med Chem Lett. 1998 Nov 3;8(21):3053-8.

Orally active indole N-oxide PDE4 inhibitors.

Author information

1
Rhône-Poulenc Rorer Central Research, Collegeville, PA 19426, USA.

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 IC50's for PDE4 inhibition and excellent in vivo activity for inhibition of TNF-alpha 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.

PMID:
9873675
DOI:
10.1016/s0960-894x(98)00572-1
[Indexed for MEDLINE]

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