کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1377858 | 981989 | 2006 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and monoamine transporter affinity of new 2β-carbomethoxy-3β-[aryl or heteroaryl]phenyltropanes
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and monoamine transporter affinity of new 2β-carbomethoxy-3β-[aryl or heteroaryl]phenyltropanes Synthesis and monoamine transporter affinity of new 2β-carbomethoxy-3β-[aryl or heteroaryl]phenyltropanes](/preview/png/1377858.png)
چکیده انگلیسی
A series of 16 new 2β-carbomethoxy-3β-[aryl or heteroaryl]phenyltropane derivatives was synthesized and evaluated for binding to monoamine transporters. Most of the compounds exhibited nanomolar affinity for the serotonin transporter (SERT). Four compounds (29, 14, 11, and 10) presented a particularly attractive pharmacological profile, with very high SERT affinity (Ki 0.15–0.5 nM) and selectivity versus the dopamine transporter of 25- to 77-fold.
A series of 16 new 2β-carbomethoxy-3β-[aryl or heteroaryl]phenyltropane derivatives was synthesized and evaluated for binding to monoamine transporters. Most of the compounds exhibited subnanomolar affinity for the serotonin transporter (SERT).Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 1, 1 January 2006, Pages 217–220
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 1, 1 January 2006, Pages 217–220
نویسندگان
Gilles Tamagnan, David Alagille, Xing Fu, Nora S. Kula, Ross J. Baldessarini, Robert B. Innis, Ronald M. Baldwin,