Dual inhibition of phosphodiesterase 4 and matrix metalloproteinases by an (arylsulfonyl)hydroxamic acid template.
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3',5'-Cyclic-AMP Phosphodiesterases↗
Biomedical subjects
R Labaudiniere
Publications and source records attributed to R Labaudiniere.
Orally active indole N-oxide PDE4 inhibitors.
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.
3',5'-Cyclic-AMP Phosphodiesterases↗
The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I.
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.
3',5'-Cyclic-AMP Phosphodiesterases↗
Quaternary substituted PDE IV inhibitors II: the synthesis and in vitro evaluation of a novel series of gamma-lactams.
This communication describes the synthesis and in vitro evaluation of a novel potent series of phosphodiesterase type (IV) (PDE IV) inhibitors. Several of the quaternary substituted lactams presented possess low nanomolar IC50's for PDE IV inhibition.
3',5'-Cyclic-AMP Phosphodiesterases↗
Parallel solid-phase synthesis of peptidyl Michael acceptors.
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Journal Article↗
Polymer-supported tetrafluorophenol: a new activated resin for chemical library synthesis.
A new tetrafluorophenol activated resin that facilitates the use of 19F NMR to quantitate loading is presented. This new resin provides a useful tool for acylation, and a novel activated polymeric sulfonate ester to generate sulfonamides. This activated resin reacts with a wide scope of N-nucleophiles including primary and secondary amines, and anilines. This new activated resin methodology provides a powerful tool for pure single-compound library synthesis.
Journal Article↗
Synthesis of a new fluoro-Wang resin for solid-phase reaction monitoring by 19F NMR spectroscopy.
A new fluoro-Wang resin is presented which facilitates solid-phase reaction monitoring using 19F NMR. The resin is easily synthesized and amenable to scale-up. The method described herein compliments single-bead FT-IR and 13C NMR techniques. This method allows monitoring of solid-phase reactions even if the resin bound intermediate is unstable to the cleavage conditions. In addition, this is a useful tool to study reaction kinetics on the solid phase.
Journal Article↗