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Carboxylate bioisosteres of gabapentin |
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| 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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