Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis
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DOI：
10.1016/j.bmcl.2009.03.007
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发表时间：
2009-04-15
影响因子：
2.7
通讯作者：
Plattner, Jacob J.
中科院分区：
文献类型：
--
作者：
Akama, Tsutomu;Baker, Stephen J.;Plattner, Jacob J.
合成了一系列苯氧基苯并氧杂硼杂环戊烯，并筛选了它们对PDE 4和细胞因子释放的抑制活性。5-（4-氰基苯氧基）-2，3-二氢-1-羟基-2，1-苯并氧杂硼杂环戊烯（AN 2728）在体外和体内均表现出强效活性。该化合物目前正在临床开发用于银屑病的局部治疗，并正在寻求用于特应性皮炎的局部治疗。(C)2009爱思唯尔有限公司保留所有权利。
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.