Discovery of novel and potent benzhydryl-tropane trypanocides highly selective for Trypanosoma cruzi
Details
Publication Year 2010-03-15,Volume 20,Issue #6,Page 1816-1818
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Publication Type
Journal Article
Abstract
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 EC(50) 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.
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Keywords
CHAGAS-DISEASE; INHIBITORS; CHEMOTHERAPY
Terms of Use/Rights Notice
Refer to copyright notice on published article.


Creation Date: 2010-03-15 12:00:00
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