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

…, V Hernandez, H Zhou, V Sanders, Y Freund…

Index: Akama, Tsutomu; Baker, Stephen J.; Zhang, Yong-Kang; Hernandez, Vincent; Zhou, Huchen; Sanders, Virginia; Freund, Yvonne; Kimura, Richard; Maples, Kirk R.; Plattner, Jacob J. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 8 p. 2129 - 2132

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Citation Number: 93

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.