کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1372032 | 981865 | 2010 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Remote functionalization of SCH 39166: Discovery of potent and selective benzazepine dopamine D1 receptor antagonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A series of novel benzazepine derived dopamine D1 antagonists have been discovered. These compounds are highly potent at D1 and showed excellent selectivity over D2 and D4 receptors. SAR studies revealed that a variety of functional groups are tolerated on the D-ring of known tetracyclic benzazepine analog 2, SCH 39166, leading to compounds with nanomolar potency at D1 and good selectivity over D2-like receptors.
A series of highly potent dopamine D1 antagonists have been discovered. All compounds showed excellent selectivity over other dopaminergic receptors. Compound 8j showed a modestly improved PK profile than SCH 39166.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 3, 1 February 2010, Pages 832–835
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 3, 1 February 2010, Pages 832–835
نویسندگان
T.K. Sasikumar, Duane A. Burnett, William J. Greenlee, Michelle Smith, Ahmad Fawzi, Hongtao Zhang, Jean E. Lachowicz,