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Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Apr 15; Vol. 19 (8), pp. 2129-32. Date of Electronic Publication: 2009 Mar 09. - Publication Year :
- 2009
-
Abstract
- 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.
- Subjects :
- Administration, Topical
Animals
Anti-Inflammatory Agents, Non-Steroidal administration & dosage
Boron Compounds administration & dosage
Bridged Bicyclo Compounds, Heterocyclic administration & dosage
Dermatitis, Atopic pathology
Dermatologic Agents administration & dosage
Edema drug therapy
Edema pathology
Humans
Mice
Psoriasis pathology
Structure-Activity Relationship
U937 Cells
Anti-Inflammatory Agents, Non-Steroidal chemistry
Boron Compounds chemistry
Bridged Bicyclo Compounds, Heterocyclic chemistry
Dermatitis, Atopic drug therapy
Dermatologic Agents chemistry
Psoriasis drug therapy
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 19
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 19303290
- Full Text :
- https://doi.org/10.1016/j.bmcl.2009.03.007