کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1367478 | 981635 | 2006 | 5 صفحه PDF | دانلود رایگان |
![عکس 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 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](/preview/png/1367478.png)
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
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 5, 1 March 2006, Pages 1207–1211