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

被引：174

作者：

Akama, Tsutomu ^{[1
]}

Baker, Stephen J. ^{[1
]}

Zhang, Yong-Kang ^{[1
]}

Hernandez, Vincent ^{[1
]}

Zhou, Huchen ^{[1
]}

Sanders, Virginia ^{[1
]}

Freund, Yvonne ^{[1
]}

Kimura, Richard ^{[1
]}

Maples, Kirk R. ^{[1
]}

Plattner, Jacob J. ^{[1
]}

机构：

[1] Anacor Pharmaceut Inc, Palo Alto, CA 94303 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 08期

关键词：

Anti-inflammatory; Phosphodiesterase; Oxaborole; Psoriasis; Atopic dermatitis; PDE4; INHIBITORS;

D O I：

10.1016/j.bmcl.2009.03.007

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

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. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：2129 / 2132

页数：4

共 12 条

[1]

Baeumer Wolfgang, 2007, Inflammation & Allergy Drug Targets, V6, P17, DOI 10.2174/187152807780077318

[2]

Identification of a novel boron-containing antibacterial agent (AN0128) with anti-inflammatory activity, for the potential treatment of cutaneous diseases [J].