Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents
ACS Medicinal Chemistry Letters2010Vol. 1(4), pp. 165–169
Citations Over TimeTop 10% of 2010 papers
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 R. Freund, Maha Abdulla, Kean-Hooi Ang, Joseline Ratnam, James H. McKerrow, Robert T. Jacobs, Huchen Zhou, Jacob J. Plattner
Abstract
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 IC50 values as low as 0.02 μg/mL and in vivo efficacy in acute murine infection models against Tryapnosoma brucei.
Related Papers
- → Comparison of an in vitro method and an in vivo method of Giardia excystation(1992)23 cited
- → IN VITRO SPECIFICITY AND IN VIVO ACTIVITY OF ANTIMACROPHAGE SERUM(1974)4 cited
- → Actin Organization as an in Vitro Assay for Tumorigenicity(1982)2 cited
- [Pharmacodynamic study of the in vitro clonogenic assay--with reference to dose levels].(1988)
- The release of the marked insulin J125 from ointment in vitro and in vivo.(1993)