Synthesis and biological evaluation of 5-carbamoyl-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors.

doi:10.1016/j.bmc.2013.09.013

Paper

Synthesis and biological evaluation of 5-carbamoyl-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors.

Published Nov 15, 2013 · Taiji Goto, Akiko Shiina, T. Yoshino

Bioorganic & medicinal chemistry

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17

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Abstract

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Non-RCT

Animal Study

Study Snapshot

5-carbamoyl-2-phenylpyrimidine derivatives show potent PDE4 inhibitory activity and anti-inflammatory properties against LPS-induced pulmonary neutrophilia in mice.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis and biological evaluation of 5-carbamoyl-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors.

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References

Identification of the fused bicyclic 4-amino-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors.

Fused bicyclic 4-amino-2-phenylpyrimidine derivatives show potent PDE4 inhibitory activity and show potential anti-inflammatory properties in mice.

Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease

Roflumilast improves lung function and reduces exacerbation frequency in COPD patients, offering a new treatment option for chronic bronchitis.

Roflumilast

Roflumilast significantly improves forced expiratory volume in 1 second (FEV1) and reduces COPD exacerbation rates in patients with severe COPD, with an acceptable tolerability profile.

Roflumilast: first phosphodiesterase 4 inhibitor approved for treatment of COPD

Roflumilast, a selective phosphodiesterase 4 inhibitor, improves lung function and reduces exacerbations in patients with more severe COPD, offering an oral treatment option.

PDE4 inhibitors: a review of current developments (2005 – 2009)

PDE4 inhibitors have shown promising clinical development since 2005, but systemic side effects remain a challenge, with roflumilast showing the best progress.

Citations

PDE4 Inhibitors: Profiling Hits through the Multitude of Structural Classes

PDE4 inhibitors show potential as therapeutic agents for treating respiratory diseases and autoimmune disorders, with potential for development through various chemical classes and structural aspects.

Advances in the development of phosphodiesterase-4 inhibitors.

PDE4 inhibitors have shown progress in development over the last decade, but their therapeutic potential for COPD and psoriasis remains hindered by emesis side effects.

Research developments in the syntheses, anti-inflammatory activities and structure–activity relationships of pyrimidines

Recent developments in pyrimidine synthesis and anti-inflammatory effects suggest potential for developing new anti-inflammatory agents with minimal toxicity.

Advances in the development of phosphodiesterase-4 inhibitors.

PDE4 inhibitors show promise as therapeutics for various diseases, with potential for further development and approval in the near future.

Construction of piperidine-2,4-dione-type azaheterocycles and their application in modern drug development and natural product synthesis.

Piperidine-2,4-dione-type azaheterocycles offer high synthetic and medicinal potential for creating pharmaceutically relevant compounds and natural products.