کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1395728 | 1501134 | 2014 | 11 صفحه PDF | دانلود رایگان |
• 23 new potent alpha 7 nAChR ligands were synthesized.
• 2 tropane derivatives exhibited a strong affinity (Ki = 13 and 14 nM).
• One 18F radiolabelled compound was obtained.
• Ex vivo biodistribution in rats was determined.
In this report, we describe the synthesis of a novel library of α7 nAChR ligands based on the modulation of the quinuclidine, quinazoline and tropane moieties. Spirane derivatives were newly synthesized under stereo specific 1,3 dipolar cylcoadditions. Only amide derivatives bonded efficiently to the receptor with Ki measured between 14 and 133 nM. The best fluorinated candidate was selected and radiolabeled. The potent [18F]4 PET tracer was evaluated in rats and its brain accumulation quantified.
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Journal: European Journal of Medicinal Chemistry - Volume 82, 23 July 2014, Pages 214–224