Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Experiment Videos

Benzofuran based PDE4 inhibitors.

D G McGarry1, J R Regan, F A Volz

  • 1Department of Medicinal Chemistry, Rhône Poulenc Rorer, Collegeville, PA 19426, USA.

Bioorganic & Medicinal Chemistry
|July 31, 1999
PubMed
Summary
This summary is machine-generated.

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Dyrk1a inhibition with the Novel Compound DYR533: A Cross-Disease Therapeutic Strategy Targeting Amyloidosis, Tau Pathogenesis, and Neuroinflammation.

bioRxiv : the preprint server for biology·2026
Same author

Behavioural intervention to promote the uptake of planned care in urgent dental care attenders: a feasibility randomised controlled trial.

BMC oral health·2024
Same author

Behavioural intervention to promote the uptake of planned care in urgent dental care attenders: study protocol for the RETURN randomised controlled trial.

Trials·2022
Same author

BMI- and age-related associations with mortality from COVID-19.

Anaesthesia·2021
Same author

Combination Fillings.

The Dental register·2021
Same author

The Gold Inlay Not Easily Made.

The Dental register·2021
Same journal

Transport specificity of FpvA and FpvB for pyoverdine-antibiotic conjugates in Pseudomonas aeruginosa.

Bioorganic & medicinal chemistry·2026
Same journal

Design and engineering of μO-conotoxin MfVIA mutants to enhance Na<sub>V</sub>1.8 inhibition and analgesic efficacy in inflammatory pain.

Bioorganic & medicinal chemistry·2026
Same journal

Recent advances in Camptothecin-derived antibody-drug conjugates.

Bioorganic & medicinal chemistry·2026
Same journal

CDK4/6-targeted therapy: From clinical inhibitors to emerging strategies to overcome resistance.

Bioorganic & medicinal chemistry·2026
Same journal

Coumarin-sulfonamide hybrids as PKM2 activators induce metabolic reprogramming and suppress ovarian cancer cell growth.

Bioorganic & medicinal chemistry·2026
Same journal

Recent advances in the development of small-molecule drugs based on covalent reversible inhibitors.

Bioorganic & medicinal chemistry·2026
See all related articles

Replacing a key structure in phosphodiesterase 4 (PDE4) inhibitors with a benzofuran unit alters their activity. This modification can either boost or significantly decrease PDE4 inhibition depending on the specific application.

Area of Science:

  • Medicinal Chemistry
  • Organic Synthesis
  • Enzyme Inhibition

Background:

  • Phosphodiesterase 4 (PDE4) enzymes play crucial roles in inflammatory processes.
  • Many existing PDE4 inhibitors feature a 3,4-dialkoxyphenyl substructure.
  • Modifications to core inhibitor structures are essential for optimizing therapeutic potential.

Purpose of the Study:

  • To investigate the impact of replacing the 3,4-dialkoxyphenyl group with a 2-alkyl-7-methoxybenzofuran unit in PDE4 inhibitors.
  • To evaluate the resulting changes in phosphodiesterase 4 inhibitory activity.
  • To conduct an in vitro structure-activity relationship (SAR) study on novel benzofuran-based compounds.

Main Methods:

  • Synthesis of novel compounds incorporating the 2-alkyl-7-methoxybenzofuran moiety.

Related Experiment Videos

  • In vitro enzymatic assays to determine phosphodiesterase 4 inhibitory activity.
  • Structure-activity relationship analysis of the synthesized benzofuran derivatives.

    • Main Results:

    • The substitution of the 3,4-dialkoxyphenyl substructure with the 2-alkyl-7-methoxybenzofuran unit led to variable effects on PDE4 inhibitory activity.
    • In some cases, the substitution enhanced PDE4 inhibition, while in others, it caused substantial reductions.
    • An in vitro SAR study identified key features influencing the activity of the 4-(2-heteroaryl-ethyl)-benzoiurans series.

    Conclusions:

    • The 2-alkyl-7-methoxybenzofuran unit represents a viable, albeit system-dependent, alternative to the traditional 3,4-dialkoxyphenyl substructure in PDE4 inhibitor design.
    • Understanding the SAR of these novel benzofuran-based compounds is critical for future drug development efforts targeting PDE4.
    • Further research is warranted to fine-tune these inhibitors for specific therapeutic applications.