加巴喷丁的羧酸盐生物电子等排体。
Carboxylate bioisosteres of gabapentin.
作者信息
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
机构信息
Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA.
出版信息
Bioorg Med Chem Lett. 2006 May 1;16(9):2333-6. doi: 10.1016/j.bmcl.2005.05.016. Epub 2005 Jun 8.
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.
已经制备了一系列与加巴喷丁1结构相关的羧酸盐生物电子等排体。当羧酸盐被四氮唑取代时，该基团被α2-δ蛋白识别。对α2-δ结合化合物14a和14b的进一步表征显示，其在体外和体内的功能活性模式与加巴喷丁1相似。
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