کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1367478 981635 2006 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of novel hexahydro-pyrido[3′,2′:4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT2C receptor agonists
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and biological evaluation of novel hexahydro-pyrido[3′,2′:4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT2C receptor agonists
چکیده انگلیسی

Further lead optimization efforts on previously described 1,2,3,4,10,10a-hexahydro-1H-pyrazino[1,2-a]indoles led to the new class of 5,5a,6,7,8,9-hexahydro-pyrido[3′,2′:4,5]pyrrolo[1,2-a]pyrazines culminating in the discovery of (5aR,9R)-2-[(cyclopropylmethoxy)methyl]-5,5a,6,7,8,9-hexahydro-9-methyl-pyrido[3′, 2′:4,5]pyrrolo[1,2-a]pyrazine 18 as a potent, full 5-HT2C receptor agonist with an outstanding selectivity profile and excellent hERG and phospholipidosis properties.

A novel series of chiral 5,5a,6,7,8,9-hexahydro-9-methyl-pyrido[3′,2′:4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT2C receptor agonists has been discovered. Several analogues had low potential to induce phospholipidosis in vitro and showed low affinity for the hERG potassium channel.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 5, 1 March 2006, Pages 1207–1211
نویسندگان
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