| Literature DB >> 16361098 |
Hans G F Richter1, D R Adams, A Benardeau, M J Bickerdike, J M Bentley, T J Blench, I A Cliffe, C Dourish, P Hebeisen, G A Kennett, A R Knight, C S Malcolm, P Mattei, A Misra, J Mizrahi, N J T Monck, J-M Plancher, S Roever, J R A Roffey, S Taylor, S P Vickers.
Abstract
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.Entities:
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Year: 2005 PMID： 16361098 DOI： 10.1016/j.bmcl.2005.11.083
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823