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. Article

Richter, Hans GF, Adams, DR, Benardeau, A et al. (2006). 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. . BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 16(5), 1207-1211. 10.1016/j.bmcl.2005.11.083

cited authors

  • Richter, Hans GF; Adams, DR; Benardeau, A; Bickerdike, MJ; Bentley, JM; Blench, TJ; Cliffe, IA; Dourish, C; Hebeisen, P; Kennett, GA; Knight, AR; Malcolm, CS; Mattei, P; Misra, A; Mizrahi, J; Monck, NJT; Plancher, J-M; Roever, S; Roffey, JRA; Taylor, S; Vickers, SP

authors

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.

publication date

  • March 1, 2006

webpage

published in

keywords

  • Animals
  • CHO Cells
  • Cricetinae
  • Humans
  • Hydroxylation
  • Molecular Structure
  • Phospholipids
  • Pyrazines
  • Pyrroles
  • Receptor, Serotonin, 5-HT2C
  • Serotonin 5-HT2 Receptor Agonists
  • Structure-Activity Relationship

Location

  • England

Digital Object Identifier (DOI)

start page

  • 1207

end page

  • 1211

volume

  • 16

issue

  • 5