Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 23, Pages 9948-9956Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.10.036
Keywords
AMPA potentiator; Allosteric modulation; Cognitive enhancer
Funding
- National Fund for Scientific Research, Belgium
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Taking into account structure-activity relationships obtained with our previous series, new diversely substituted 1,2,4-pyridothiadiazine 1,1-dioxides were designed to obtain novel AMPA potentiators. The aim of this work was focused on the improvement of lipophilicity, which is well known as a critical parameter to obtain in vivo active central nervous system agents. For this purpose, two positions on the pyridine ring were privileged to insert selected groups. Among the synthesized compounds emerged 7-chloro-4-ethyl-3,4-dihydro-2H-pyrido[2,3-e]-[1,2,4]- thiadiazine 1,1-dioxide (12d), which was evaluated in two memory tests in Wistar rats and showed cognition enhancing effects after intraperitoneal injection at doses as low as 0.3 mg/kg. (c) 2008 Elsevier Ltd. All rights reserved.
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