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
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists
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
نویسندگان
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