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新型大麻素能配体的2-取代冰片药效基团的合成与表征

Synthesis and characterization of 2-substituted bornane pharmacophores for novel cannabinergic ligands.

作者信息

Duclos Richard I, Lu Dai, Guo Jianxin, Makriyannis Alexandros

机构信息

Center for Drug Discovery, Northeastern University, 360 Huntington Avenue, 116 Mugar Life Sciences Building, Boston, MA 02115, USA.

出版信息

Tetrahedron Lett. 2008 Sep 22;49(39):5587-5589. doi: 10.1016/j.tetlet.2008.07.029.

Abstract

Analogously to the fenchyl and adamantyl groups, the bornyl and epimeric isobornyl groups are compact lipophilic substituents that can be incorporated into drug design to improve pharmacological or physicochemical properties. Methods are reported for the synthesis and characterization of 2-substituted norbornanes and bornanes that can serve as novel cannabinergic ligand intermediates.

摘要

与葑基和金刚烷基类似,冰片基和差向异构异冰片基是紧密的亲脂性取代基,可引入药物设计中以改善药理或物理化学性质。本文报道了可作为新型大麻素能配体中间体的2-取代降冰片烷和冰片烷的合成及表征方法。

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