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Carboxylate bioisosteres of pregabalin

JB Schwarz, NL Colbry, Z Zhu, B Nichelson…

文献索引:Schwarz, Jacob B.; Colbry, Norman L.; Zhu, Zhijian; Nichelson, Brian; Barta, Nancy S.; Lin, Kristin; Hudack, Raymond A.; Gibbons, Sian E.; Galatsis, Paul; DeOrazio, Russell J.; Manning, David D.; Vartanian, Mark G.; Kinsora, Jack J.; Lotarski, Susan M.; Li, Zheng; Dickerson, Melvin R.; El-Kattan, Ayman; Thorpe, Andrew J.; Donevan, Sean D.; Taylor, Charles P.; Wustrow, David J. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 13 p. 3559 - 3563

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被引用次数: 12

摘要

Several β-amino tetrazole analogs of gabapentin 1 and pregabalin 2 were prepared by one of two convergent, highly efficient routes, and their affinity for the α2–δ protein examined. Two select compounds with potent affinity for α2–δ, 8a and 16a, were subsequently tested in vivo in an audiogenic seizure model and found to elicit protective effects.