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Synthesis and biological evaluation of novel hexahydro-pyrido[3′,2′:4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT2C receptor agonists by Hans G.F. Richter; 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 is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Synthesis and biological evaluation of novel hexahydro-pyrido[3′,2′:4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT2C receptor agonists about?

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 0 ,2 0 :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 0 , 2 0 :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.

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Author

Hans G.F. Richter; 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

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)

Published

2006

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)