Department of Chemistry, University of New Orleans, New Orleans, LA 70148, USA.
Bioorg Med Chem Lett. 2013 Aug 1;23(15):4404-7. doi: 10.1016/j.bmcl.2013.05.071. Epub 2013 May 29.
A series of 3-aryl-3-arylmethoxy-azetidines were synthesized and evaluated for binding affinities at dopamine and serotonin transporters. The 3-aryl-3-arylmethoxyazetidines were generally SERT selective with the dichloro substituted congener 7c (Ki=1.0 nM) and the tetrachloro substituted derivative 7i (Ki=1.3 nM) possessing low nanomolar affinity for the SERT. The 3-(3,4-dichlorophenyl-3-phenylmethoxyazetidine (7g) exhibited moderate affinity at both DAT and SERT transporters and suggests that substitution of the aryl rings can be used to tune the mononamine transporter affinity.
一系列 3-芳基-3-芳甲氧基氮杂环丁烷被合成并评估了它们与多巴胺和血清素转运体的结合亲和力。3-芳基-3-芳甲氧基氮杂环丁烷通常对 SERT 具有选择性，其中二氯取代的同系物 7c（Ki=1.0 nM）和四氯取代的衍生物 7i（Ki=1.3 nM）对 SERT 具有低纳摩尔亲和力。3-（3,4-二氯苯基-3-苯甲氧基氮杂环丁烷（7g）在 DAT 和 SERT 转运体上均表现出中等亲和力，这表明芳基环的取代可以用于调节单胺转运体的亲和力。
