کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1363720 | 981520 | 2009 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists](/preview/png/1363720.png)
چکیده انگلیسی
A novel series of annulated tricyclic compounds was synthesized and evaluated as NMDA/NR2B antagonists. Structure–activity development was directed towards in vitro optimization of NR2B activity and selectivity over the hERG K+ channel. Preferred compounds were subsequently evaluated for selectivity in an α1-adrenergic receptor binding counter-screen and a cell-based assay of NR2B activity.
A novel series of annulated tricyclic compounds was synthesized and evaluated as NMDA/NR2B antagonists. Compound (−)23b was identified as one which showed good separation of NR2B and hERG activities.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 17, 1 September 2009, Pages 5132–5135
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 17, 1 September 2009, Pages 5132–5135
نویسندگان
Charles J. McIntyre, John A. McCauley, Bohumil Bednar, Rodney A. Bednar, John W. Butcher, David A. Claremon, Michael E. Cunningham, Roger M. Freidinger, Stanley L. Gaul, Carl F. Homnick, Ken S. Koblan, Scott D. Mosser, Joseph J. Romano,