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

被引：69

作者：

Baker, Stephen J.

Akama, Tsutomu

Zhang, Yong-Kang

Sauro, Vittorio

Pandit, Chetan

Singh, Rajeshwar

Kully, Maureen

Khan, Jehangir

Plattner, Jacob J.

Benkovic, Stephen J.

Lee, Ving

Maples, Kirk R.

机构：

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

[2] NAEJA Pharmaceut Inc, Edmonton, AB T6E 5V2, Canada

[3] Penn State Univ, Wartik Lab 414, University Pk, PA 16802 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 23期

关键词：

atopic dermatitis; antibacterial activity; borinic acid picolinate ester; structure-activity relationship;

D O I：

10.1016/j.bmcl.2006.08.130

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of borinic acid picolinate esters were synthesized and screened for their minimum inhibitory concentration (MIC) against Gram-positive and -negative bacteria. Our lead compounds were then screened for anti-inflammatory activity. From these studies, we identified 3-hydroxypyridine-2-carbonyloxy-bis(3-chloro-4-methylphenyl)borane (2g, AN0128) as having the best combination of anti-bacterial and anti-inflammatory activities. This compound is now in clinical development for dermatological conditions. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：5963 / 5967

页数：5

共 6 条

[1] Identification of borinic esters as inhibitors of bacterial cell growth and bacterial methyltransferases, CcrM and MenH [J].