Synthesis and structure–activity relationship study of substituted caffeate esters as antinociceptive agents modulating the TREK-1 channel

…, H Deokar, J Busserolles, F Lesage, A Eschalier…

Index: Rodrigues, Nuno; Bennis, Khalil; Vivier, Delphine; Pereira, Vanessa; Chatelain, Franck C.; Chapuy, Eric; Deokar, Hemantkumar; Busserolles, Jerome; Lesage, Florian; Eschalier, Alain; Ducki, Sylvie European Journal of Medicinal Chemistry, 2014 , vol. 75, p. 391 - 402

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Citation Number: 11

Abstract

Abstract The TWIK-related K+ channel, TREK-1, has recently emerged as an attractive therapeutic target for the development of a novel class of analgesic drugs. It has been reported that TREK-1−/− mice were more sensitive than wild-type mice to painful stimuli, suggesting that activation of TREK-1 could result in pain inhibition. Here we report the synthesis of a series of substituted caffeate esters (12a–u) based on the hit compound ...