氟化 2-芳基环丙基-1-胺 - 一类新型的 sigma 受体配体。
Fluorinated 2-Arylcyclopropan-1-amines - A new class of sigma receptor ligands.
机构信息
Organisch-Chemisches Institut, Universität Münster, Corrensstr. 40, 48149 Münster, Germany.
Institut für Pharmazeutische und Medizinische Chemie, Universität Münster, Corrensstr. 48, 48149 Münster, Germany.
出版信息
Bioorg Med Chem. 2020 Nov 15;28(22):115726. doi: 10.1016/j.bmc.2020.115726. Epub 2020 Sep 1.
Stereoisomeric 2-aryl-2-fluoro-cyclopropan-1-amines have been discovered as a new class of σ receptor ligands showing different selectivity for the two subtypes of the receptor. Generally, compounds substituted in 4-position are much more active than corresponding 3-substituted isomers. trans-2-Fluoro-2-(4-methoxyphenyl)cyclopropan-1-amine (19a) was the most potent (K = 4.8 nM) σ receptor ligand, while cis-2-fluoro-2-(4-trifluoromethylphenyl)cyclopropan-1-amine (20b) was the most potent (K = 95 nM) σ receptor ligand.
手性 2-芳基-2-氟环丙基-1-胺已被发现为一类新型 σ 受体配体，对受体的两种亚型表现出不同的选择性。一般来说，4-位取代的化合物比相应的 3-位取代异构体活性更高。反式-2-氟-2-(4-甲氧基苯基)环丙基-1-胺（19a）是最有效的（K=4.8 nM）σ 受体配体，而顺式-2-氟-2-(4-三氟甲基苯基)环丙基-1-胺（20b）是最有效的（K=95 nM）σ 受体配体。
Zotero 插件