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

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-hexahydr...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-03, Vol.16 (5), p.1207-1211
Hauptverfasser:	Richter, Hans G F, Adams, D R, Benardeau, A, Bickerdike, M J, Bentley, J M, Blench, T J, Cliffe, I A, Dourish, C, Hebeisen, P, Kennett, G A, Knight, A R, Malcolm, C S, Mattei, P, Misra, A, Mizrahi, J, Monck, N J T, Plancher, J-M, Roever, S, Roffey, J R A, Taylor, S, Vickers, S P
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals CHO Cells Cricetinae Humans Hydroxylation Molecular Structure Phospholipids - pharmacology Pyrazines - chemical synthesis Pyrazines - chemistry Pyrazines - pharmacology Pyrroles - chemistry Receptor, Serotonin, 5-HT2C - genetics Receptor, Serotonin, 5-HT2C - metabolism Serotonin 5-HT2 Receptor Agonists Structure-Activity Relationship
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Zusammenfassung:	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-HT(2C) receptor agonist with an outstanding selectivity profile and excellent hERG and phospholipidosis properties.
ISSN:	0960-894X