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

Synthesis and biological evaluation of novel hexahydro- pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT sub(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-hexahy...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2006-01, Vol.16 (5), p.1207-1211
Hauptverfasser: Richter, Hans GF, Adams, DR, Benardeau, A, Bickerdike, MJ, Bentley, J M, Blench, T J, Cliffe, IA, Dourish, C, Hebeisen, P, Kennett, G A, Knight, A R, Malcolm, C S, Mattei, P, Misra, A, Mizrahi, J, Monck, NJT, Plancher, J-M, Roever, S, Roffey, JRA, Taylor, S, Vickers, S P
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Sprache:eng
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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 sub(2C) receptor agonist with an outstanding selectivity profile and excellent hERG and phospholipidosis properties.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.11.083