Author/Authors :
Steven M. Bromidge، نويسنده , , Steven Dabbs، نويسنده , , David T. Davies، نويسنده , , Susannah Davies، نويسنده , , D. Malcolm Duckworth، نويسنده , , Ian T. Forbes، نويسنده , , Angela Gadre، نويسنده , , Peter Ham، نويسنده , , Graham E. Jones، نويسنده , , Frank D. King، نويسنده , , Damian V. Saunders، نويسنده , , Kevin M. Thewlis، نويسنده , , Deepa Vyas، نويسنده , , Thomas P. Blackburn، نويسنده , , Vicky Holland، نويسنده , , Guy A. Kennett، نويسنده , , Graham J. Riley، نويسنده , , Martyn D. Wood، نويسنده ,
Abstract :
A model series of 5-HT2C antagonists have been prepared by rapid parallel synthesis. These N-substituted phenyl-N′-pyridin-3-yl ureas were found to have a range of 5-HT2C receptor affinities and selectivities over the closely related 5-HT2A receptor. Extrapolation of simple SAR, derived from this set of compounds, to the more active but synthetically more complex 1-(3-pyridyl-carbamoyl)indoline series allowed us to target optimal substitution patterns and identify potent and selective 5-HT2C/2B antagonists.
Keywords :
anxiolytics , Receptors , Antidepressants , 5-HT2C/2B antagonists
