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

Tsutomu Akama,Stephen J Baker,Yong-Kang Zhang,Vincent Hernandez,Huchen Zhou,Virginia Sanders,Yvonne Freund,Richard Kimura,Kirk R Maples,Jacob J Plattner

doi:10.1016/j.bmcl.2009.03.007

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

Tsutomu Akama, Stephen J Baker + Show 8 more

https://doi.org/10.1016/j.bmcl.2009.03.007

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Journal: Bioorganic & Medicinal Chemistry Letters	Publication Date: Mar 9, 2009
Citations: 225

#Topical Treatment Of Atopic Dermatitis #Topical Treatment Of Psoriasis + Show 8 more

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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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