an2728 has been researched along with Edema* in 3 studies
3 other study(ies) available for an2728 and Edema
| Article | Year |
|---|---|
Design, synthesis and biological evaluation of novel benzoxaborole derivatives as potent PDE4 inhibitors for topical treatment of atopic dermatitis.
In this work, a series of structurally novel benzoxaborole derivatives were designed, synthesized and biologically evaluated as PDE4 inhibitors for battling atopic dermatitis (AD). Among them, the majority exhibited superior PDE4B inhibitory activities to that of the lead compound Crisaborole, an approved PDE4 inhibitor. In particular, 72, the most potent PDE4B inhibitor throughout this series, displayed 136-fold improved enzymatic activity (IC Topics: Animals; Boron Compounds; Calcitriol; Cyclic Nucleotide Phosphodiesterases, Type 4; Dermatitis, Atopic; Dose-Response Relationship, Drug; Drug Design; Edema; Female; Guinea Pigs; Male; Mice; Mice, Inbred ICR; Molecular Docking Simulation; Molecular Structure; Phosphodiesterase 4 Inhibitors; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Tetradecanoylphorbol Acetate | 2021 |
Design and synthesis of boron-containing PDE4 inhibitors using soft-drug strategy for potential dermatologic anti-inflammatory application.
PDE4 inhibitors are a validated approach as anti-inflammatory agents but are limited by systemic side effects including emesis. We report a soft-drug strategy incorporating a carboxylic ester group into boron-containing PDE4 inhibitors leading to the discovery of a series of benzoxaborole compounds with good potency (for example IC(50)=47 nM of compound 2) and low emetic activity. These compounds are intended for dermatological use further limiting possible systemic side effects. Topics: Animals; Anti-Inflammatory Agents; Boron; Cyclic Nucleotide Phosphodiesterases, Type 4; Ear; Edema; Humans; Mice; Phosphodiesterase 4 Inhibitors | 2010 |
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.
A series of phenoxy benzoxaboroles were synthesized and screened for their inhibitory activity against PDE4 and cytokine release. 5-(4-Cyanophenoxy)-2,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2728) showed potent activity both in vitro and in vivo. This compound is now in clinical development for the topical treatment of psoriasis and being pursued for the topical treatment of atopic dermatitis. Topics: Administration, Topical; Animals; Anti-Inflammatory Agents, Non-Steroidal; Boron Compounds; Bridged Bicyclo Compounds, Heterocyclic; Dermatitis, Atopic; Dermatologic Agents; Edema; Humans; Mice; Psoriasis; Structure-Activity Relationship; U937 Cells | 2009 |