Design, optimization, and in vivo evaluation of a series of pyridine derivatives with dual NK1 antagonism and SERT inhibition for the treatment of depression

A series of substituted pyridines, ether linked to a phenylpiperidine core were optimized for dual NK1/SERT affinity. Optimization based on NK1/SERT binding affinities, and minimization of off-target ion channel activity lead to the discovery of compound 44. In vivo evaluation of 44 in the gerbil fo...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2013-01, Vol.23 (2), p.407-411
Hauptverfasser: Gillman, Kevin W., Parker, Michael F., Silva, Mark, Degnan, Andrew P., Tora, George O., Lodge, Nicholas J., Li, Yu-Wen, Lelas, Snjezana, Taber, Matthew, Krause, Rudolf G., Bertekap, Robert L., Newton, Amy E., Pieschl, Rick L., Lengyel, Kelly D., Johnson, Kim A., Taylor, Sarah J., Bronson, Joanne J., Macor, John E.
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Sprache:eng
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