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Fluorinated 2-Arylcyclopropan-1-amines – A new class of sigma receptor ligands
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2020-09-01 , DOI: 10.1016/j.bmc.2020.115726 Benjamin Schinor 1 , Svenja Hruschka 1 , Constantin G Daniliuc 1 , Dirk Schepmann 2 , Bernhard Wünsch 2 , Günter Haufe 3
中文翻译：
氟化2-Arylcyclopropan-1-amines –新型sigma受体配体
更新日期：2020-09-11
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2020-09-01 , DOI: 10.1016/j.bmc.2020.115726 Benjamin Schinor 1 , Svenja Hruschka 1 , Constantin G Daniliuc 1 , Dirk Schepmann 2 , Bernhard Wünsch 2 , Günter Haufe 3
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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 (Ki = 4.8 nM) σ1 receptor ligand, while cis-2-fluoro-2-(4-trifluoromethylphenyl)cyclopropan-1-amine (20b) was the most potent (Ki = 95 nM) σ2 receptor ligand.
中文翻译：
氟化2-Arylcyclopropan-1-amines –新型sigma受体配体
立体异构体2-芳基-2-氟-环丙烷-1-胺已被发现是一类新的σ受体配体，对受体的两种亚型表现出不同的选择性。通常，在4-位取代的化合物比相应的3-取代异构体具有更高的活性。反式-2-氟-2-（4-甲氧基苯基）环丙烷-1-胺（19A）是最有效的（ķ我 = 4.8 nm）的σ 1个受体配体，而顺式-2-氟-2-（4-三氟甲基苯基基）环丙烷-1-胺（20B）是最有效的（ķ我 = 95 nM）的σ 2受体配体。
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