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Bioorg Med Chem Lett. 1998 Jul 21;8(14):1867-72.

The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I.

Author information

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

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 IC50's for PDEIV inhibition. In vivo activities determined from measurement of serum TNF-alpha levels in LPS challenged mice (mouse endotoxemia model) are also reported.

PMID:
9873449
DOI:
10.1016/s0960-894x(98)00324-2
[Indexed for MEDLINE]

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