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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.

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.
AuthorsTsutomu Akama, Stephen J Baker, Yong-Kang Zhang, Vincent Hernandez, Huchen Zhou, Virginia Sanders, Yvonne Freund, Richard Kimura, Kirk R Maples, Jacob J Plattner
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 19 Issue 8 Pg. 2129-32 (Apr 15 2009) ISSN: 1464-3405 [Electronic] England
PMID19303290 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Anti-Inflammatory Agents, Non-Steroidal
  • Boron Compounds
  • Bridged Bicyclo Compounds, Heterocyclic
  • Dermatologic Agents
  • crisaborole
Topics
  • Administration, Topical
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal (administration & dosage, chemistry)
  • Boron Compounds (administration & dosage, chemistry)
  • Bridged Bicyclo Compounds, Heterocyclic (administration & dosage, chemistry)
  • Dermatitis, Atopic (drug therapy, pathology)
  • Dermatologic Agents (administration & dosage, chemistry)
  • Edema (drug therapy, pathology)
  • Humans
  • Mice
  • Psoriasis (drug therapy, pathology)
  • Structure-Activity Relationship
  • U937 Cells

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