Synthesis and biological evaluation of novel hexahydro-pyrido [3′, 2′: 4, 5] pyrrolo [1, 2-a] pyrazines as potent and selective 5-HT 2C receptor agonists

…, C Dourish, P Hebeisen, GA Kennett, AR Knight…

文献索引：Richter, Hans G. F.; Adams; Benardeau; Bickerdike; Bentley; Blench; Cliffe; Dourish; Hebeisen; Kennett; Knight; Malcolm; Mattei; Misra; Mizrahi; Monck; Plancher; Roever; Roffey; Taylor; Vickers Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 5 p. 1207 - 1211

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被引用次数: 30

摘要

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 ...