Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 11, Pages 2916-2919Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.04.096
Keywords
Sleeping sickness; Trypanosomiasis; S-Adenosylmethionine decarboxylase (AdoMetDC); Inhibitor; Blood brain barrier; Purine
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Funding
- DNDi
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Modification of the structure of trypanosomal AdoMetDC inhibitor 1 (MDL73811) resulted in the identification of a new inhibitor 7a, which features a methyl substituent at the 8-position. Compound 7a exhibits improved potencies against both the trypanosomal AdoMetDC enzyme and parasites, and better blood brain barrier penetration than 1. (C) 2009 Published by Elsevier Ltd.
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