Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
A series of 1-(1-pyrrolo(iso)quinolinyl)-2-propylamines was synthesised and evaluated as 5-HT(2C) receptor agonists for the treatment of obesity. The general methods of synthesis of the precursor indoles are described. The functional efficacy and radioligand binding data for the compounds at 5-HT(2) receptor subtypes are reported. The analogue which showed the highest 5-HT(2C) binding affinity (27, 1.6nM) was found to be successful in reducing food intake in rats.
Adams
David R
DR
Vernalis plc, Oakdene Court, 613 Reading Road, Winnersh, Wokingham, Berkshire RG41 5UA, UK.
Bentley
Jonathan M
JM
Benwell
Karen R
KR
Bickerdike
Michael J
MJ
Bodkin
Corinna D
CD
Cliffe
Ian A
IA
Dourish
Colin T
CT
George
Ashley R
AR
Kennett
Guy A
GA
Knight
Antony R
AR
Malcolm
Craig S
CS
Mansell
Howard L
HL
Misra
Anil
A
Quirk
Kathleen
K
Roffey
Jonathan R A
JR
Vickers
Steven P
SP
D000818:Animals; D019440:Anti-Obesity Agents / Q000494:pharmacology; D004195:Disease Models, Animal; D004435:Eating / Q000187:drug effects*; D007546:Isoquinolines / Q000737:chemistry / Q000494:pharmacology*; D011758:Pyrroles / Q000737:chemistry; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D011869:Radioligand Assay; D051381:Rats; D058826:Serotonin 5-HT2 Receptor Agonists; D017366:Serotonin Receptor Agonists / Q000494:pharmacology*
D019440:Anti-Obesity Agents; D007546:Isoquinolines; D011758:Pyrroles; D011804:Quinolines; D058826:Serotonin 5-HT2 Receptor Agonists; D017366:Serotonin Receptor Agonists; C039109:isoquinoline