The γ-lactam moiety is present in a large number of natural and non-natural biologically active compounds. The range of biological activities covered by these compounds is very broad. Functionalized γ-lactams are thus of high interest and have great potential in medicinal chemistry. This review provides a description of the title compounds by focusing on their synthesis, natural sources and biological activities.

Biologically active γ-lactams: synthesis and natural sources.

The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) 
processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.

Substituted oxazolidinones and their use in the field of blood coagulation

Phosphodiesterase (PDE) enzymes are responsible for the inactiviation of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). Phosphodiesterase 4 (PDE4) is a cAMP specific phosphodiesterase expressed in inflammatory cells such as eosinophils. Inhibition of PDE4 results in an elevation of cAMP in these cells, which in turn downregulates the inflammatory response. The anti-inflammatory effects of PDE4 inhibitors have been well documented both in vitro and in vivo in a range of animal models. The potential use of PDE4 inhibitors as anti-inflammatory agents for the treatment of diseases such as asthma, chronic obstructive pulmonary disease (COPD) and multiple sclerosis (MS), has received considerable attention from the pharmaceutical industry but to date, there are no selective PDE4 inhibitors on the market. Early PDE4 inhibitors, such as rolipram suffered from dose limiting side effects, including nausea and emesis, which severely restricted their therapeutic utility. Second gener...

Update on the therapeutic potential of PDE4 inhibitors.

Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.

Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs.

Phosphodiesterase 4 inhibitors

: Both enantiomers of rolipram ( 1 ) have been prepared in large quantity from a commonintermediate rac- 3-(3’-cyclopentyloxy-4’-methoxy)phenyl-4-nitro butyric acid ( 6 ), which was resolved byway of the two readily separable diastereoisomeric amides obtained with ( S )-(−)-phenylethylamine. Reductionof the nitro group and intramolecular transamidation gave ( R )-(−)- 1 and ( S )-(+)- 1 , respectively. CD spectraof both enantiomers of rolipram are reported and discussed. Both enantiomers of rolipram presented the samepotency of inhibitory activity against recombinant cyclic-AMP-selective phosphodiesterase (PDE4) subtypes. Keywords: Rolipram, phosphodiesterase, circular dichroism (CD) spectra, enantiodivergent synthesis. Introduction Rolipram ( 1 ) is a compound with varied biologicalactivity. In particular, attention has been drawn to theemetic [1], antiinflammatory [2], immunosupressant [3],antidepressive [4,5], putative antiparkinsonian [6], andneuroprotective [7] effects. The best characterisedbiochemical activity of

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Edmond Bacher

Papers

Enantiodivergent Synthesis of (R)- and (S)-Rolipram

Studies towards the synthesis of 16α-carboxyprednisolones. Chemistry of fused bromoisoxazolines

N-arylrolipram derivatives as potent and selective PDE4 inhibitors

Synthesis of N-Arylrolipram Derivatives — Potent and Selective Phosphodiesterase-IV Inhibitors — by Copper-Catalyzed Lactam—Aryl Halide Coupling.

Synthesis of n-arylrolipram derivatives - potent and selective phosphodiesterase-iv inhibitors: by copper catalyzed lactam-aryl halide coupling