Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents

Dazhong Ding; Yaxue Zhao; Qingqing Meng; Dongsheng Xie; Bakela Nare; Daitao Chen; Cyrus J. Bacchi; Nigel Yarlett; Yong-Kang Zhang; Vincent Hernandez; Yi Xia; Yvonne Freund; Maha Abdulla; Kean-Hooi Ang; Joseline Ratnam; James H. McKerrow; Robert T. Jacobs; Huchen Zhou; Jacob J. Plattner

doi:10.1021/ml100013s

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Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents

Journal article

Peer reviewed

Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents

Dazhong Ding, Yaxue Zhao, Qingqing Meng, Dongsheng Xie, Bakela Nare, Daitao Chen, Cyrus J. Bacchi, Nigel Yarlett, Yong-Kang Zhang, Vincent Hernandez, …

ACS medicinal chemistry letters, Vol.1(4), pp.165-169

08/07/2010

DOI: https://doi.org/10.1021/ml100013s

PMCID: PMC4007846

PMID: 24900190

Abstract

African trypanosomiasis

benzoxaborole

Letter

Tryapnosoma brucei

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 μg/mL and in vivo efficacy in acute murine infection models against Tryapnosoma brucei .

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Title: Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents
Creators - without role: Dazhong Ding - Shanghai Jiao Tong University
Yaxue Zhao - Shanghai Jiao Tong University
Qingqing Meng - Shanghai Jiao Tong University
Dongsheng Xie - Shanghai Jiao Tong University
Bakela Nare - Scynexis
Daitao Chen - Scynexis
Cyrus J. Bacchi - Pace University
Nigel Yarlett - Pace University
Yong-Kang Zhang - Anacor Pharmaceuticals
Vincent Hernandez - Anacor Pharmaceuticals
Yi Xia - Anacor Pharmaceuticals
Yvonne Freund - Anacor Pharmaceuticals
Maha Abdulla - University of California, San Francisco
Kean-Hooi Ang - University of California, San Francisco
Joseline Ratnam - University of California, San Francisco
James H. McKerrow - University of California, San Francisco
Robert T. Jacobs - Scynexis
Huchen Zhou - Shanghai Jiao Tong University
Jacob J. Plattner - Anacor Pharmaceuticals
Publication Details: ACS medicinal chemistry letters, Vol.1(4), pp.165-169
Publisher: American Chemical Society
Identifiers: 9948627908331
Academic Unit: King Saud University
Language: English
Resource Type: Journal article