Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 4, Pages 1214-1217Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.12.070
Keywords
Organophosphorus agents; Acetylcholinesterase; Fluorinated pyridinium oxime; Oxime reactivators
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Funding
- Korea Foundation for International Cooperation of Science AMP
- Technology (KICOS) through Korean Ministry of Education Science Technology [K20702000710-08B1200-01910]
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For the purpose of developing new oxime reactivators of acetylcholinesterases (AChE) that have been inhibited by organophosphorus agents, emphasis was given to the finding that the lipophilic nature of fluorinated compounds is responsible for their enhanced transport across the blood brain barrier (BBB). As a result, we have designed and synthesized the fluorinated oxime derivatives, which quantum mechanical calculations suggest should have a greater lipophilicity and BBB permeability than their non-fluorinated analogs. Among the compounds explored in this study, 4 was found to have the highest potency for reactivation of paraoxon-inhibited housefly (HF) AChE. (C) 2008 Elsevier Ltd. All rights reserved.
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