Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents

被引：72

作者：

Ding, Dazhong ^{[1
,2
]}

Zhao, Yaxue ^{[1
,2
]}

Meng, Qingqing ^{[1
,2
]}

Xie, Dongsheng ^{[1
,2
]}

Nare, Bakela ^{[3
]}

Chen, Daitao ^{[3
]}

Bacchi, Cyrus J. ^{[4
]}

Yarlett, Nigel ^{[4
]}

Zhang, Yong-Kang ^{[5
]}

Hernandez, Vincent ^{[5
]}

Xia, Yi ^{[5
]}

Freund, Yvonne ^{[5
]}

Abdulla, Maha ^{[6
,7
]}

Ang, Kean-Hooi ^{[6
,7
]}

Ratnam, Joseline ^{[6
,7
]}

McKerrow, James H. ^{[6
,7
]}

Jacobs, Robert T. ^{[3
]}

Zhou, Huchen ^{[1
,2
]}

Plattner, Jacob J. ^{[5
]}

机构：

[1] Shanghai Jiao Tong Univ, Sch Pharm, Shanghai 200240, Peoples R China

[2] Shanghai Jiao Tong Univ, E Inst Chem Biol, Shanghai 200240, Peoples R China

[3] SCYNEXIS Inc, Res Triangle Pk, NC 27709 USA

[4] Pace Univ, Haskins Lab, New York, NY 10038 USA

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

[6] Univ Calif San Francisco, Small Mol Discovery Ctr, San Francisco, CA 94158 USA

[7] Univ Calif San Francisco, Sandler Ctr Basic Res Parasit Dis, San Francisco, CA 94158 USA

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2010年 / 1卷 / 04期

基金：

美国国家科学基金会;

关键词：

Tryapnosoma brucei; African trypanosomiasis; benzoxaborole; DRUG DISCOVERY; DISEASES;

D O I：

10.1021/ml100013s

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the discovery of benzoxaborole antitrypanosomal agents and their structure activity relationships on central linkage groups and different substitution patterns in the sulfur-linked series. The compounds showed in vitro growth inhibition IC(50) values as low as 0.02 mu g/mL and in vivo efficacy in acute murine infection models against nryapnosoma brucei.

引用

页码：165 / 169

页数：5

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