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Carboxylate bioisosteres of gabapentin
Authors:Burgos-Lepley Carmen E  Thompson Lisa R  Kneen Clare O  Osborne Simon A  Bryans Justin S  Capiris Thomas  Suman-Chauhan Nirmala  Dooley David J  Donovan Cindy M  Field Mark J  Vartanian Mark G  Kinsora Jack J  Lotarski Susan M  El-Kattan Ayman  Walters Karen  Cherukury Madhu  Taylor Charles P  Wustrow David J  Schwarz Jacob B
Affiliation:Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA.
Abstract:A series of carboxylate bioisosteres of structures related to gabapentin 1 have been prepared. When the carboxylate was replaced by a tetrazole, this group was recognized by the alpha2-delta protein. Further characterization of alpha2-delta binding compounds 14a and 14b revealed a similar pattern of functional in vitro and in vivo activity to gabapentin 1.
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