کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373815 | 981906 | 2010 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis, and biological evaluation of new monoamine reuptake inhibitors with potential therapeutic utility in depression and pain
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Design, synthesis, and biological evaluation of new monoamine reuptake inhibitors with potential therapeutic utility in depression and pain Design, synthesis, and biological evaluation of new monoamine reuptake inhibitors with potential therapeutic utility in depression and pain](/preview/png/1373815.png)
چکیده انگلیسی
Two new series of monoamine triple reuptake inhibitors (TRIs) have been discovered through scaffold homologation of our recently reported series of 3,3-disubstituted pyrrolidine TRIs. The regioisomeric 2- and 3-ketopyrrolidines demonstrated high levels of potency against all three monoamine transporters as well as good human in vitro stability, low drug–drug interaction potential and a decreased propensity for hERG channel binding. Representative compounds from these series displayed good in vivo pharmacokinetics and high monoamine receptor occupancies which are indicators of good brain penetration.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 18, 15 September 2010, Pages 5559–5566
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 18, 15 September 2010, Pages 5559–5566
نویسندگان
Matthew C. Lucas, Robert J. Weikert, David S. Carter, Hai-Ying Cai, Robert Greenhouse, Pravin S. Iyer, Clara J. Lin, Eun Kyung Lee, Ann Marie Madera, Amy Moore, Kerem Ozboya, Ryan C. Schoenfeld, Sandra Steiner, Yansheng Zhai, Stephen M. Lynch,