期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 6, 页码 1816-1818出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.02.022
关键词
Trypanosoma; Chagas disease
资金
- drugs for neglected diseases initiative (DNDi)
- Victorian State Government OISS
- NHRMC IRIISS [361646]
A benzhydryl tropinone oxime that is potently toxic to Trypanosoma cruzi has been previously identified. An SAR investigation determined that no part of the original compound was superfluous and all early SAR probes led to significant drops in activity. The only alteration that could be achieved without loss of activity was replacement of the aryl chloride substituent with chloro homologues. This led to the discovery of a trifluoromethyl-containing analogue with an EC50 against T. cruzi of 30 nM and a cytotoxicity selectivity index of over 1000 relative to rat skeletal myoblast L-6 cells. (C) 2010 Elsevier Ltd. All rights reserved.
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