Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis

  • Bioorg Med Chem Lett. 2009 Apr 15;19(8):2129-32. doi: 10.1016/j.bmcl.2009.03.007.
Tsutomu Akama  1 ,  Stephen J Baker ,  Yong-Kang Zhang ,  Vincent Hernandez ,  Huchen Zhou ,  Virginia Sanders ,  Yvonne Freund ,  Richard Kimura ,  Kirk R Maples ,  Jacob J Plattner
Affiliations
PMID: 19303290 DOI: 10.1016/j.bmcl.2009.03.007
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.

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